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

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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

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10 mM * 1 mL in DMSO ￥550 In-stock
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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.

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