Pitavastatin D4(Synonyms: NK-104 D4)

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。

Pitavastatin D4 (Synonyms: NK-104 D4)

Pitavastatin D4 (NK-104 D4) 是 Pitavastatin 的氘代物。Pitavastatin 是一种有效的 HMG-CoA 还原酶抑制剂。

Pitavastatin D4(Synonyms: NK-104 D4)

Pitavastatin D4 Chemical Structure

CAS No. : 2070009-71-9

规格 是否有货
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生物活性

Pitavastatin D4 (NK-104 D4) is deuterium labeled Pitavastatin. Pitavastatin is a potent HMG-CoA reductase inhibitor.

分子量

425.49

Formula

C25H20D4FNO4

CAS 号

2070009-71-9

中文名称

匹伐他汀 D4

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.

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

Pitavastatin D4(Synonyms: NK-104 D4)

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。

Pitavastatin D4 (Synonyms: NK-104 D4)

Pitavastatin D4 (NK-104 D4) 是 Pitavastatin 的氘代物。Pitavastatin 是一种有效的 HMG-CoA 还原酶抑制剂。

Pitavastatin D4(Synonyms: NK-104 D4)

Pitavastatin D4 Chemical Structure

CAS No. : 2070009-71-9

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

Pitavastatin D4 (NK-104 D4) is deuterium labeled Pitavastatin. Pitavastatin is a potent HMG-CoA reductase inhibitor.

分子量

425.49

Formula

C25H20D4FNO4

CAS 号

2070009-71-9

中文名称

匹伐他汀 D4

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.

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

Pitavastatin-d4 hemicalcium(Synonyms: NK-104-d4 hemicalcium; Pitavastatin-d4 hemicalcium)

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。

Pitavastatin-d4 hemicalcium (Synonyms: NK-104-d4 hemicalcium; Pitavastatin-d4 hemicalcium)

Pitavastatin-d4 (hemicalcium) 是 Pitavastatin (Calcium) 氘代物。Pitavastatin Calcium (NK-104 hemicalcium) 是有效的羟甲基戊二酰-CoA (HMG-CoA) 还原酶抑制剂。Pitavastatin Calcium 在 HepG2 细胞中抑制乙酸合成胆固醇的 IC50 为 5.8 nM。Pitavastatin Calcium 是一种高效的肝细胞低密度脂蛋白胆固醇 (LDL-C) 受体诱导剂。具有抗癌活性。

Pitavastatin-d4 hemicalcium(Synonyms: NK-104-d4 hemicalcium; Pitavastatin-d4 hemicalcium)

Pitavastatin-d4 hemicalcium Chemical Structure

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250 mg   询价  
500 mg   询价  

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生物活性

Pitavastatin-d4 (hemicalcium) is deuterium labeled Pitavastatin (Calcium). Pitavastatin Calcium (NK-104 hemicalcium) is a potent hydroxymethylglutaryl-CoA (HMG-CoA) reductase inhibitor. Pitavastatin Calcium (NK-104 hemicalcium) inhibits cholesterol synthesis from acetic acid with an IC50 of 5.8 nM in HepG2 cells. Pitavastatin Calcium is an efficient hepatocyte low-density lipoprotein-cholesterol (LDL-C) receptor inducer. Anti-cancer activity[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

444.52

Formula

C25H19D4FNO.1/2Ca2+

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]. Mukhtar RY, et al. Pitavastatin. Int J Clin Pract. 2005 Feb;59(2):239-52.

    [3]. Kajinami K, et al. Pitavastatin: efficacy and safety profiles of a novel synthetic HMG-CoA reductase inhibitor. Cardiovasc Drug Rev. 2003 Fall;21(3):199-215.

    [4]. de Wolf E, et al.Dietary geranylgeraniol can limit the activity of pitavastatin as a potential treatment for drug-resistant ovarian cancer.Sci Rep. 2017 Jul 14;7(1):5410.

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

Pitavastatin(Synonyms: 匹伐他汀; NK-104)

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。

Pitavastatin (Synonyms: 匹伐他汀; NK-104)

Pitavastatin (NK-104) 是有效的羟甲基戊二酰-CoA (HMG-CoA) 还原酶抑制剂。Pitavastatin 在 HepG2 细胞中抑制乙酸合成胆固醇的 IC50 为 5.8 nM。Pitavastatin 是一种高效的肝细胞低密度脂蛋白胆固醇 (LDL-C) 受体诱导剂。具有抗癌活性。

Pitavastatin(Synonyms: 匹伐他汀; NK-104)

Pitavastatin Chemical Structure

CAS No. : 147511-69-1

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

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Pitavastatin 的其他形式现货产品:

Pitavastatin Calcium

生物活性

Pitavastatin (NK-104) is a potent hydroxymethylglutaryl-CoA (HMG-CoA) reductase inhibitor. Pitavastatin inhibits cholesterol synthesis from acetic acid with an IC50 of 5.8 nM in HepG2 cells. Pitavastatin is an efficient hepatocyte low-density lipoprotein-cholesterol (LDL-C) receptor inducer. Anti-cancer activity.

体外研究
(In Vitro)

Pitavastatin inhibits the growth of a panel of ovarian cancer cells, including those considered most likely to represent HGSOC, grown as a monolayers (IC50=0.4-5 μM) or as spheroids (IC50 = 0.6-4 μM)[4]
Pitavastatin (1 μM; 48 hours ) induces apoptosis, evidenced by the increased activity of executioner caspases-3,7 as well as caspase-8 and caspase-9 in Ovcar-8 cells and Ovcar-3 cells[4].
Pitavastatin (1 μM, 48 hours) caused PARP cleavage in Ovcar-8 cells[4].

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

Western Blot Analysis[1]

Cell Line: Ovcar-8 cells
Concentration: 1 μM
Incubation Time: 48 hours
Result: Induced PARP cleavage.

体内研究
(In Vivo)

Pitavastatin (59 mg/kg; p.o.; twice daily for 28 days) caused significant tumour regression[4].

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

Animal Model: 4 week old female NCR Nu/Nu female mice (bearing Ovcar-4 tumours)[4]
Dosage: 59 mg/kg
Administration: p.o.; twice daily for 28 days
Result: Caused significant tumour regression.

Clinical Trial

分子量

421.46

Formula

C25H24FNO4

CAS 号

147511-69-1

中文名称

匹伐他汀

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]. Morikawa S, et al. Relative induction of mRNA for HMG CoA reductase and LDL receptor by five different HMG-CoA reductase inhibitors in cultured human cells. J Atheroscler Thromb. 2000;7(3):138-44.

    [2]. Katsuki S, et al. Nanoparticle-mediated delivery of pitavastatin inhibits atherosclerotic plaque destabilization/rupture in mice by regulating the recruitment of inflammatory monocytes. Circulation. 2014 Feb 25;129(8):896-906.

    [3]. Tajiri K, et al. Pitavastatin regulates helper T-cell differentiation and ameliorates autoimmune myocarditis in mice. Cardiovasc Drugs Ther. 2013 Oct;27(5):413-24.

    [4]. Hamano T, et al. Pitavastatin decreases tau levels via the inactivation of Rho/ROCK. Neurobiol Aging. 2012 Oct;33(10):2306-20.

    [5]. de Wolf E, et al.Dietary geranylgeraniol can limit the activity of pitavastatin as a potential treatment for drug-resistant ovarian cancer.Sci Rep. 2017 Jul 14;7(1):5410.

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

Pitavastatin Calcium(Synonyms: 匹伐他汀钙; NK-104 hemicalcium; Pitavastatin hemicalcium)

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。

Pitavastatin Calcium (Synonyms: 匹伐他汀钙; NK-104 hemicalcium; Pitavastatin hemicalcium) 纯度: 99.45%

Pitavastatin Calcium (NK-104 hemicalcium) 是有效的羟甲基戊二酰-CoA (HMG-CoA) 还原酶抑制剂。Pitavastatin Calcium 在 HepG2 细胞中抑制乙酸合成胆固醇的 IC50 为 5.8 nM。Pitavastatin Calcium 是一种高效的肝细胞低密度脂蛋白胆固醇 (LDL-C) 受体诱导剂。具有抗癌活性。

Pitavastatin Calcium(Synonyms: 匹伐他汀钙; NK-104 hemicalcium; Pitavastatin hemicalcium)

Pitavastatin Calcium Chemical Structure

CAS No. : 147526-32-7

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
10 mg ¥500 In-stock
50 mg ¥1200 In-stock
100 mg ¥2000 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Pitavastatin Calcium 相关产品

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生物活性

Pitavastatin Calcium (NK-104 hemicalcium) is a potent hydroxymethylglutaryl-CoA (HMG-CoA) reductase inhibitor. Pitavastatin Calcium (NK-104 hemicalcium) inhibits cholesterol synthesis from acetic acid with an IC50 of 5.8 nM in HepG2 cells. Pitavastatin Calcium is an efficient hepatocyte low-density lipoprotein-cholesterol (LDL-C) receptor inducer. Anti-cancer activity[1][2][3].

体外研究
(In Vitro)

Pitavastatin Calcium inhibits the growth of a panel of ovarian cancer cells, including those considered most likely to represent HGSOC, grown as a monolayers (IC50 = 0.4-5 μM) or as spheroids (IC50=0.6-4 μM)[3].
Pitavastatin Calcium (1 μM; 48 hours ) induces apoptosis, evidenced by the increased activity of executioner caspases-3,7 as well as caspase-8 and caspase-9 in Ovcar-8 cells and Ovcar-3 cells[3].
Pitavastatin (1 μM, 48 hours) caused PARP cleavage in Ovcar-8 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.

Western Blot Analysis[3]

Cell Line: Ovcar-8 cells
Concentration: 1 μM
Incubation Time: 48 hours
Result: Induced PARP cleavage.

体内研究
(In Vivo)

Pitavastatin Calcium (59 mg/kg; p.o.; twice daily for 28 days) caused significant tumour regression[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: 4 week old female NCR Nu/Nu female mice (bearing Ovcar-4 tumours)[3]
Dosage: 59 mg/kg
Administration: p.o.; twice daily for 28 days
Result: Caused significant tumour regression.

Clinical Trial

分子量

440.49

Formula

C25H23Ca0.5FNO4

CAS 号

147526-32-7

中文名称

匹伐他汀钙

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

溶解性数据
In Vitro: 

DMSO : ≥ 50 mg/mL (113.51 mM)

* “≥” 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 2.2702 mL 11.3510 mL 22.7020 mL
5 mM 0.4540 mL 2.2702 mL 4.5404 mL
10 mM 0.2270 mL 1.1351 mL 2.2702 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 and light)。-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 (5.68 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.68 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 (5.68 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.68 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 (5.68 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.68 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]. Mukhtar RY, et al. Pitavastatin. Int J Clin Pract. 2005 Feb;59(2):239-52.

    [2]. Kajinami K, et al. Pitavastatin: efficacy and safety profiles of a novel synthetic HMG-CoA reductase inhibitor. Cardiovasc Drug Rev. 2003 Fall;21(3):199-215.

    [3]. de Wolf E, et al.Dietary geranylgeraniol can limit the activity of pitavastatin as a potential treatment for drug-resistant ovarian cancer.Sci Rep. 2017 Jul 14;7(1):5410.

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