Pitavastatin(Synonyms: 匹伐他汀; NK-104)

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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

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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.

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