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

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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

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10 mM * 1 mL in DMSO ¥550 In-stock
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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.

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