标签归档：amlodipine

Amlodipine-d4 maleate(Synonyms: 马来酸氨氯地平 d4 (马来酸盐))

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Amlodipine-d4 maleate (Synonyms: 马来酸氨氯地平 d4 (马来酸盐))

Amlodipine-d4 maleate 是 Amlodipine maleate 的氘代物。Amlodipine maleate 是二氢吡啶类钙通道 (calcium channel) 阻滞剂，作为一种具有口服活性的抗心绞痛试剂 (antianginal agent)。Amlodipine maleate 阻断了电压依赖性的 L 型钙通道，从而抑制了钙离子内流。Amlodipine maleate 可用于高血压和癌症的研究。

Amlodipine-d4 maleate(Synonyms: 马来酸氨氯地平 d4 (马来酸盐))

Amlodipine-d4 maleate Chemical Structure

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

Amlodipine-d4 maleate is the deuterium labeled Amlodipine maleate. Amlodipine maleate is a dihydropyridine calcium channel blocker, acts as an orally active antianginal agent. Amlodipine maleate blocks the voltage-dependent L-type calcium channels, thereby inhibiting the initial influx of calcium. Amlodipine maleate can be used for the research of high blood pressure and cancer[1][2][3].

体外研究
(In Vitro)

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

528.97

Formula

C24H25D4ClN2O9
中文名称

马来酸氨氯地平 d4 (马来酸盐)
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

    [2]. Kishen G. Bulsara, et al. Amlodipine.

    [3]. Haria M, et al. Amlodipine. A reappraisal of its pharmacological properties and therapeutic use in cardiovascular disease [published correction appears in Drugs 1995 Nov;50(5):896]. Drugs. 1995;50(3):560-586.

    [4]. Yoshida J, et, al. Antitumor effects of amlodipine, a Ca2+ channel blocker, on human epidermoid carcinoma A431 cells in vitro and in vivo. Eur J Pharmacol. 2004 May 25;492(2-3):103-12.

    [5]. Okuyama Y, et, al. The effects of anti-hypertensive drugs and the mechanism of hypertension in vascular smooth muscle cell-specific ATP2B1 knockout mice. Hypertens Res. 2018 Feb;41(2):80-87.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

Amlodipine maleate(Synonyms: 马来酸氨氯地平)

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Amlodipine maleate (Synonyms: 马来酸氨氯地平) 纯度: 99.85%

Amlodipine maleate 是二氢吡啶类钙通道 (calcium channel) 阻滞剂，作为一种具有口服活性的抗心绞痛试剂 (antianginal agent)。Amlodipine maleate 阻断了电压依赖性的 L 型钙通道，从而抑制了钙离子内流。Amlodipine maleate 可用于高血压和癌症的研究。

Amlodipine maleate(Synonyms: 马来酸氨氯地平)

Amlodipine maleate Chemical Structure

CAS No. : 88150-47-4

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ￥550 In-stock
500 mg ￥500 In-stock
1 g ￥700 In-stock
5 g ￥2200 In-stock
10 g   询价  
50 g   询价  

* Please select Quantity before adding items.

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生物活性

Amlodipine maleate is a dihydropyridine calcium channel blocker, acts as an orally active antianginal agent. Amlodipine maleate blocks the voltage-dependent L-type calcium channels, thereby inhibiting the initial influx of calcium. Amlodipine maleate can be used for the research of high blood pressure and cancer[1][2][3].

IC50 & Target

L-type calcium channel[1]
体外研究
(In Vitro)

Amlodipine maleate (20-40 μM; 48 h) reduces BrdU incorporation to 68.6% and 26.3% at concentrations of 20 and 30 μM in A431 cells, respectively[3].
Amlodipine maleate (30 μM; pretreated for 1 h) significantly attenuates the uridine 5′-triphosphate (UTP)-induced increases of [Ca2+]i in A431 cells[3].
Amlodipine maleate (30 μM) inhibits the store-operated Ca2+influx evoked by Thapsigargin in Fluo-3-loaded cells[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

Amlodipine maleate (5 mg/kg/day; s.c. for 2 weeks) significantly decreases systolic blood pressure (SBP) in VSMC ATP2B1 KO mice[4].
Amlodipine maleate (10 mg/kg; i.p. once daily for 20 days) causes a significant retardation of tumor growth and prolongs the survival of A431 tumor-bearing mice[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: ATP2B1loxP/loxP mice[4]
Dosage: 5 mg/kg/day
Administration: Subcutaneously implanted osmotic pump for 2 weeks
Result: Significantly decreased the blood pressure.

Clinical Trial

分子量

524.95

Formula

C24H29ClN2O9
CAS 号

88150-47-4
中文名称

马来酸氨氯地平；氨氯地平马来酸盐
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
溶解性数据
In Vitro: 

DMSO : 120 mg/mL (228.59 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.9049 mL 9.5247 mL 19.0494 mL
5 mM 0.3810 mL 1.9049 mL 3.8099 mL
10 mM 0.1905 mL 0.9525 mL 1.9049 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 1.71 mg/mL (3.26 mM); Clear solution

    此方案可获得 ≥ 1.71 mg/mL (3.26 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 17.1 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 1.71 mg/mL (3.26 mM); Clear solution

    此方案可获得 ≥ 1.71 mg/mL (3.26 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 17.1 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
  • 3.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 1.71 mg/mL (3.26 mM); Clear solution

    此方案可获得 ≥ 1.71 mg/mL (3.26 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 17.1 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Kishen G. Bulsara, et al. Amlodipine.

    [2]. Haria M, et al. Amlodipine. A reappraisal of its pharmacological properties and therapeutic use in cardiovascular disease [published correction appears in Drugs 1995 Nov;50(5):896]. Drugs. 1995;50(3):560-586.

    [3]. Yoshida J, et, al. Antitumor effects of amlodipine, a Ca2+ channel blocker, on human epidermoid carcinoma A431 cells in vitro and in vivo. Eur J Pharmacol. 2004 May 25;492(2-3):103-12.

    [4]. Okuyama Y, et, al. The effects of anti-hypertensive drugs and the mechanism of hypertension in vascular smooth muscle cell-specific ATP2B1 knockout mice. Hypertens Res. 2018 Feb;41(2):80-87.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

Amlodipine mesylate

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Amlodipine mesylate 

Amlodipine mesylate 是一种抗心绞痛药和具有口服活性二氢吡啶钙通道（calcium channel）阻滞剂，通过阻断电压依赖性的 L 型钙通道，从而抑制钙离子内流。Amlodipine mesylate 可用于高血压和癌症的研究。

Amlodipine mesylate

Amlodipine mesylate Chemical Structure

CAS No. : 246852-12-0

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Amlodipine mesylate 的其他形式现货产品:

Amlodipine Amlodipine maleate Amlodipine besylate

生物活性

Amlodipine mesylate, an antianginal agent and an orally active dihydropyridine calcium channel blocker, works by blocking the voltage-dependent L-type calcium channels, thereby inhibiting the initial influx of calcium. Amlodipine mesylate can be used for the research of high blood pressure and cancer[1][2][3].

IC50 & Target

L-type calcium channel

 

体外研究
(In Vitro)

Amlodipine mesylate (20-40 μM; 48 h) reduces BrdU incorporation to 68.6% and 26.3% at concentrations of 20 and 30 μM in A431 cells, respectively[3].
Amlodipine mesylate (30 μM; pretreated for 1 h) significantly attenuates the uridine 5′-triphosphate (UTP)-induced increases of [Ca2+]i in A431 cells[3].
Amlodipine mesylate (30 μM) inhibits the store-operated Ca2+influx evoked by Thapsigargin in Fluo-3-loaded cells[3].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

Amlodipine mesylate (5 mg/kg/day; s.c. for 2 weeks) significantly decreases systolic blood pressure (SBP) in VSMC ATP2B1 KO mice[4].
Amlodipine mesylate (10 mg/kg; i.p. once daily for 20 days) causes a significant retardation of tumor growth and prolongs the survival of A431 tumor-bearing mice[3].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: ATP2B1loxP/loxP mice[4]
Dosage: 5 mg/kg/day
Administration: Subcutaneously implanted osmotic pump for 2 weeks
Result: Significantly decreased the blood pressure.

分子量

504.98

Formula

C21H29ClN2O8S
CAS 号

246852-12-0
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Kishen G. Bulsara, et al. Amlodipine.

    [2]. Haria M, et al. Amlodipine. A reappraisal of its pharmacological properties and therapeutic use in cardiovascular disease [published correction appears in Drugs 1995 Nov;50(5):896]. Drugs. 1995;50(3):560-586.

    [3]. Yoshida J, et, al. Antitumor effects of amlodipine, a Ca2+ channel blocker, on human epidermoid carcinoma A431 cells in vitro and in vivo. Eur J Pharmacol. 2004 May 25;492(2-3):103-12.

    [4]. Okuyama Y, et, al. The effects of anti-hypertensive drugs and the mechanism of hypertension in vascular smooth muscle cell-specific ATP2B1 knockout mice. Hypertens Res. 2018 Feb;41(2):80-87.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

Amlodipine-d4 besylate(Synonyms: Amlodipine benzenesulfonate-d4 besylate)

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Amlodipine-d4 besylate (Synonyms: Amlodipine benzenesulfonate-d4 besylate)

Amlodipine-d4 (Amlodipine (benzenesulfonate)-d4) besylate 是 Amlodipine besylate 的氘代物。Amlodipine besylate (Amlodipine benzenesulfonate) 是一种抗心绞痛剂和具有口服活性二氢吡啶钙通道阻滞剂，通过阻断电压依赖性的 L 型钙通道，从而抑制钙离子内流。Amlodipine besylate 可用于高血压和癌症的研究。

Amlodipine-d4 besylate(Synonyms: Amlodipine benzenesulfonate-d4 besylate)

Amlodipine-d4 besylate Chemical Structure

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

Amlodipine-d4 (Amlodipine (benzenesulfonate)-d4) besylate is the deuterium labeled Amlodipine besylate. Amlodipine besylate (Amlodipine benzenesulfonate), an antianginal agent and an orally active dihydropyridine calcium channel blocker, works by blocking the voltage-dependent L-type calcium channels, thereby inhibiting the initial influx of calcium. Amlodipine besylate can be used for the research of high blood pressure and cancer[1][2][3].

体外研究
(In Vitro)

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

571.08

Formula

C26H27D4ClN2O8S
中文名称

苯磺酸氨氯地平 d4 (苯磺酸盐)
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

    [2]. Kishen G. Bulsara, et al. Amlodipine.

    [3]. Haria M, et al. Amlodipine. A reappraisal of its pharmacological properties and therapeutic use in cardiovascular disease [published correction appears in Drugs 1995 Nov;50(5):896]. Drugs. 1995;50(3):560-586.

    [4]. Yoshida J, et, al. Antitumor effects of amlodipine, a Ca2+ channel blocker, on human epidermoid carcinoma A431 cells in vitro and in vivo. Eur J Pharmacol. 2004 May 25;492(2-3):103-12.

    [5]. Okuyama Y, et, al. The effects of anti-hypertensive drugs and the mechanism of hypertension in vascular smooth muscle cell-specific ATP2B1 knockout mice. Hypertens Res. 2018 Feb;41(2):80-87.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

Amlodipine-d4 besylate(Synonyms: Amlodipine benzenesulfonate-d4 besylate)

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Amlodipine-d4 besylate (Synonyms: Amlodipine benzenesulfonate-d4 besylate)

Amlodipine-d4 (Amlodipine (benzenesulfonate)-d4) besylate 是 Amlodipine besylate 的氘代物。Amlodipine besylate (Amlodipine benzenesulfonate) 是一种抗心绞痛剂和具有口服活性二氢吡啶钙通道阻滞剂，通过阻断电压依赖性的 L 型钙通道，从而抑制钙离子内流。Amlodipine besylate 可用于高血压和癌症的研究。

Amlodipine-d4 besylate(Synonyms: Amlodipine benzenesulfonate-d4 besylate)

Amlodipine-d4 besylate Chemical Structure

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

Amlodipine-d4 (Amlodipine (benzenesulfonate)-d4) besylate is the deuterium labeled Amlodipine besylate. Amlodipine besylate (Amlodipine benzenesulfonate), an antianginal agent and an orally active dihydropyridine calcium channel blocker, works by blocking the voltage-dependent L-type calcium channels, thereby inhibiting the initial influx of calcium. Amlodipine besylate can be used for the research of high blood pressure and cancer[1][2][3].

体外研究
(In Vitro)

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

571.08

Formula

C26H27D4ClN2O8S
中文名称

苯磺酸氨氯地平 d4 (苯磺酸盐)
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

    [2]. Kishen G. Bulsara, et al. Amlodipine.

    [3]. Haria M, et al. Amlodipine. A reappraisal of its pharmacological properties and therapeutic use in cardiovascular disease [published correction appears in Drugs 1995 Nov;50(5):896]. Drugs. 1995;50(3):560-586.

    [4]. Yoshida J, et, al. Antitumor effects of amlodipine, a Ca2+ channel blocker, on human epidermoid carcinoma A431 cells in vitro and in vivo. Eur J Pharmacol. 2004 May 25;492(2-3):103-12.

    [5]. Okuyama Y, et, al. The effects of anti-hypertensive drugs and the mechanism of hypertension in vascular smooth muscle cell-specific ATP2B1 knockout mice. Hypertens Res. 2018 Feb;41(2):80-87.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

Amlodipine-d4 besylate(Synonyms: Amlodipine benzenesulfonate-d4 besylate)

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Amlodipine-d4 besylate (Synonyms: Amlodipine benzenesulfonate-d4 besylate)

Amlodipine-d4 (Amlodipine (benzenesulfonate)-d4) besylate 是 Amlodipine besylate 的氘代物。Amlodipine besylate (Amlodipine benzenesulfonate) 是一种抗心绞痛剂和具有口服活性二氢吡啶钙通道阻滞剂，通过阻断电压依赖性的 L 型钙通道，从而抑制钙离子内流。Amlodipine besylate 可用于高血压和癌症的研究。

Amlodipine-d4 besylate(Synonyms: Amlodipine benzenesulfonate-d4 besylate)

Amlodipine-d4 besylate Chemical Structure

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

Amlodipine-d4 (Amlodipine (benzenesulfonate)-d4) besylate is the deuterium labeled Amlodipine besylate. Amlodipine besylate (Amlodipine benzenesulfonate), an antianginal agent and an orally active dihydropyridine calcium channel blocker, works by blocking the voltage-dependent L-type calcium channels, thereby inhibiting the initial influx of calcium. Amlodipine besylate can be used for the research of high blood pressure and cancer[1][2][3].

体外研究
(In Vitro)

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

571.08

Formula

C26H27D4ClN2O8S
中文名称

苯磺酸氨氯地平 d4 (苯磺酸盐)
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

    [2]. Kishen G. Bulsara, et al. Amlodipine.

    [3]. Haria M, et al. Amlodipine. A reappraisal of its pharmacological properties and therapeutic use in cardiovascular disease [published correction appears in Drugs 1995 Nov;50(5):896]. Drugs. 1995;50(3):560-586.

    [4]. Yoshida J, et, al. Antitumor effects of amlodipine, a Ca2+ channel blocker, on human epidermoid carcinoma A431 cells in vitro and in vivo. Eur J Pharmacol. 2004 May 25;492(2-3):103-12.

    [5]. Okuyama Y, et, al. The effects of anti-hypertensive drugs and the mechanism of hypertension in vascular smooth muscle cell-specific ATP2B1 knockout mice. Hypertens Res. 2018 Feb;41(2):80-87.

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Amlodipine-1,1,2,2-d4 maleate(Synonyms: 氨氯地平 d4 (马来酸盐))

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Amlodipine-1,1,2,2-d4 maleate (Synonyms: 氨氯地平 d4 (马来酸盐))

Amlodipine-1,1,2,2-d4 maleate 是 Amlodipine 的氘代物。Amlodipine 是一种抗心绞痛药和具有口服活性二氢吡啶钙通道阻滞剂，通过阻断电压依赖性的 L 型钙通道，从而抑制钙离子内流。Amlodipine 可用于高血压和癌症的研究。

Amlodipine-1,1,2,2-d4 maleate(Synonyms: 氨氯地平 d4 (马来酸盐))

Amlodipine-1,1,2,2-d4 maleate Chemical Structure

CAS No. : 1185246-15-4

规格 是否有货
5 mg Check price and availability
25 mg Check price and availability
50 mg Check price and availability

* Please select Quantity before adding items.

生物活性

Amlodipine-1,1,2,2-d4 maleate is the deuterium labeled Amlodipine. Amlodipine, an antianginal agent and an orally active dihydropyridine calcium channel blocker, works by blocking the voltage-dependent L-type calcium channels, thereby inhibiting the initial influx of calcium. Amlodipine can be used for the research of high blood pressure and cancer[1][2][3].

体外研究
(In Vitro)

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

528.97

Formula

C24H25D4ClN2O9
CAS 号

1185246-15-4
中文名称

氨氯地平 d4 (马来酸盐)
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

    [2]. Kishen G. Bulsara, et al. Amlodipine.

    [3]. Haria M, et al. Amlodipine. A reappraisal of its pharmacological properties and therapeutic use in cardiovascular disease [published correction appears in Drugs 1995 Nov;50(5):896]. Drugs. 1995;50(3):560-586.

    [4]. Yoshida J, et, al. Antitumor effects of amlodipine, a Ca2+ channel blocker, on human epidermoid carcinoma A431 cells in vitro and in vivo. Eur J Pharmacol. 2004 May 25;492(2-3):103-12.

    [5]. Okuyama Y, et, al. The effects of anti-hypertensive drugs and the mechanism of hypertension in vascular smooth muscle cell-specific ATP2B1 knockout mice. Hypertens Res. 2018 Feb;41(2):80-87.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

Amlodipine besylate(Synonyms: 苯磺酸氨氯地平; Amlodipine benzenesulfonate)

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Amlodipine besylate (Synonyms: 苯磺酸氨氯地平; Amlodipine benzenesulfonate) 纯度: 99.92%

Amlodipine besylate (Amlodipine benzenesulfonate) 是一种抗心绞痛剂和具有口服活性二氢吡啶钙通道阻滞剂，通过阻断电压依赖性的 L 型钙通道，从而抑制钙离子内流。Amlodipine besylate 可用于高血压和癌症的研究。

Amlodipine besylate(Synonyms: 苯磺酸氨氯地平; Amlodipine benzenesulfonate)

Amlodipine besylate Chemical Structure

CAS No. : 111470-99-6

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ￥550 In-stock
500 mg ￥500 In-stock
1 g ￥700 In-stock
5 g ￥2200 In-stock
10 g   询价  
50 g   询价  

* Please select Quantity before adding items.

Amlodipine besylate 相关产品

•相关化合物库:

  • Drug Repurposing Compound Library Plus
  • FDA-Approved Drug Library Plus
  • FDA-Approved Drug Library Mini
  • Bioactive Compound Library Plus
  • Membrane Transporter/Ion Channel Compound Library
  • Neuronal Signaling Compound Library
  • FDA-Approved Drug Library
  • Anti-Cancer Compound Library
  • Drug Repurposing Compound Library
  • Anti-Cardiovascular Disease Compound Library
  • NMPA-Approved Drug Library
  • Orally Active Compound Library
  • FDA Approved & Pharmacopeial Drug Library
  • Neuroprotective Compound Library
  • Drug-Induced Liver Injury (DILI) Compound Library
  • Rare Diseases Drug Library

生物活性

Amlodipine besylate (Amlodipine benzenesulfonate), an antianginal agent and an orally active dihydropyridine calcium channel blocker, works by blocking the voltage-dependent L-type calcium channels, thereby inhibiting the initial influx of calcium. Amlodipine besylate can be used for the research of high blood pressure and cancer[1][2][3].

IC50 & Target

L-type calcium channel[1]
体外研究
(In Vitro)

Amlodipine besylate (20-40 μM; 48 h) reduces BrdU incorporation to 68.6% and 26.3% at concentrations of 20 and 30 μM in A431 cells, respectively[3].
Amlodipine besylate (30 μM; pretreated for 1 h) significantly attenuates the uridine 5′-triphosphate (UTP)-induced increases of [Ca2+]i in A431 cells[3].
Amlodipine besylate (30 μM) inhibits the store-operated Ca2+influx evoked by Thapsigargin in Fluo-3-loaded cells[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

Amlodipine besylate (5 mg/kg/day; s.c. for 2 weeks) significantly decreases systolic blood pressure (SBP) in VSMC ATP2B1 KO mice[4].
Amlodipine besylate (10 mg/kg; i.p. once daily for 20 days) causes a significant retardation of tumor growth and prolongs the survival of A431 tumor-bearing mice[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: ATP2B1loxP/loxP mice[4]
Dosage: 5 mg/kg/day
Administration: Subcutaneously implanted osmotic pump for 2 weeks
Result: Significantly decreased the blood pressure.

Clinical Trial

分子量

567.05

Formula

C26H31ClN2O8S
CAS 号

111470-99-6
中文名称

苯磺酸氨氯地平
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
溶解性数据
In Vitro: 

DMSO : ≥ 45 mg/mL (79.36 mM)

H2O : 1 mg/mL (1.76 mM; Need ultrasonic)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.7635 mL 8.8176 mL 17.6351 mL
5 mM 0.3527 mL 1.7635 mL 3.5270 mL
10 mM 0.1764 mL 0.8818 mL 1.7635 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (4.41 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.41 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (4.41 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.41 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
  • 3.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (4.41 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (4.41 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Kishen G. Bulsara, et al. Amlodipine.

    [2]. Haria M, et al. Amlodipine. A reappraisal of its pharmacological properties and therapeutic use in cardiovascular disease [published correction appears in Drugs 1995 Nov;50(5):896]. Drugs. 1995;50(3):560-586.

    [3]. Yoshida J, et, al. Antitumor effects of amlodipine, a Ca2+ channel blocker, on human epidermoid carcinoma A431 cells in vitro and in vivo. Eur J Pharmacol. 2004 May 25;492(2-3):103-12.

    [4]. Okuyama Y, et, al. The effects of anti-hypertensive drugs and the mechanism of hypertension in vascular smooth muscle cell-specific ATP2B1 knockout mice. Hypertens Res. 2018 Feb;41(2):80-87.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

Amlodipine(Synonyms: 氨氯地平)

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Amlodipine (Synonyms: 氨氯地平) 纯度: 99.76%

Amlodipine 是一种抗心绞痛药和具有口服活性二氢吡啶钙通道阻滞剂，通过阻断电压依赖性的 L 型钙通道，从而抑制钙离子内流。Amlodipine 可用于高血压和癌症的研究。

Amlodipine(Synonyms: 氨氯地平)

Amlodipine Chemical Structure

CAS No. : 88150-42-9

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ￥550 In-stock
500 mg ￥500 In-stock
1 g ￥700 In-stock
5 g ￥2200 In-stock
10 g   询价  
50 g   询价  

* Please select Quantity before adding items.

Amlodipine 相关产品

•相关化合物库:

  • Drug Repurposing Compound Library Plus
  • FDA-Approved Drug Library Plus
  • FDA-Approved Drug Library Mini
  • Bioactive Compound Library Plus
  • Membrane Transporter/Ion Channel Compound Library
  • Neuronal Signaling Compound Library
  • FDA-Approved Drug Library
  • Anti-Cancer Compound Library
  • Drug Repurposing Compound Library
  • Anti-Cardiovascular Disease Compound Library
  • NMPA-Approved Drug Library
  • Orally Active Compound Library
  • FDA Approved & Pharmacopeial Drug Library
  • Neuroprotective Compound Library
  • Drug-Induced Liver Injury (DILI) Compound Library
  • Rare Diseases Drug Library

生物活性

Amlodipine, an antianginal agent and an orally active dihydropyridine calcium channel blocker, works by blocking the voltage-dependent L-type calcium channels, thereby inhibiting the initial influx of calcium. Amlodipine can be used for the research of high blood pressure and cancer[1][2][3].

IC50 & Target[1]

L-type calcium channel

 

体外研究
(In Vitro)

Amlodipine (20-40 μM; 48 h) reduces BrdU incorporation to 68.6% and 26.3% at concentrations of 20 and 30 μM in A431 cells, respectively[3].
Amlodipine (30 μM; pretreated for 1 h) significantly attenuates the uridine 5′-triphosphate (UTP)-induced increases of [Ca2+]i in A431 cells[3].
Amlodipine (30 μM) inhibits the store-operated Ca2+influx evoked by Thapsigargin in Fluo-3-loaded cells[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

Amlodipine (5 mg/kg/day; s.c. for 2 weeks) significantly decreases systolic blood pressure (SBP) in VSMC ATP2B1 KO mice[4].
Amlodipine (10 mg/kg; i.p. once daily for 20 days) causes a significant retardation of tumor growth and prolongs the survival of A431 tumor-bearing mice[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: ATP2B1loxP/loxP mice[4]
Dosage: 5 mg/kg/day
Administration: Subcutaneously implanted osmotic pump for 2 weeks
Result: Significantly decreased the blood pressure.

Clinical Trial

分子量

408.88

Formula

C20H25ClN2O5
CAS 号

88150-42-9
中文名称

安氯地平；阿洛地平；氨氯地平
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 120 mg/mL (293.48 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.4457 mL 12.2285 mL 24.4571 mL
5 mM 0.4891 mL 2.4457 mL 4.8914 mL
10 mM 0.2446 mL 1.2229 mL 2.4457 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 3 mg/mL (7.34 mM); Clear solution

    此方案可获得 ≥ 3 mg/mL (7.34 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 30.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 3 mg/mL (7.34 mM); Suspended solution; Need ultrasonic

    此方案可获得 3 mg/mL (7.34 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例，取 100 μL 30.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
  • 3.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 3 mg/mL (7.34 mM); Clear solution

    此方案可获得 ≥ 3 mg/mL (7.34 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 30.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Kishen G. Bulsara, et al. Amlodipine.

    [2]. Haria M, et al. Amlodipine. A reappraisal of its pharmacological properties and therapeutic use in cardiovascular disease [published correction appears in Drugs 1995 Nov;50(5):896]. Drugs. 1995;50(3):560-586.

    [3]. Yoshida J, et, al. Antitumor effects of amlodipine, a Ca2+ channel blocker, on human epidermoid carcinoma A431 cells in vitro and in vivo. Eur J Pharmacol. 2004 May 25;492(2-3):103-12.

    [4]. Okuyama Y, et, al. The effects of anti-hypertensive drugs and the mechanism of hypertension in vascular smooth muscle cell-specific ATP2B1 knockout mice. Hypertens Res. 2018 Feb;41(2):80-87.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务