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Pitavastatin Calcium

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Chemical Structure| 147526-32-7 同义名 : NK-104 hemicalcium;Pitavastatin hemicalcium;NKS 104;Itavastatin;Itabastatin;Pitavastatin (calcium salt);NK-104 calcium
CAS号 : 147526-32-7
货号 : A135712
分子式 : C50H46CaF2N2O8
纯度 : 98%
分子量 : 880.984
MDL号 : MFCD01937979
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(56.75 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 The enzyme 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA ) reductase is the rate-limiting enzyme involved in the multistep synthesis of cholesterol. Pitavastatin is a fully synthetic competitive inhibitor of HMG-CoA reductase[4]. Pitavastatin Calcium (NK-104 hemicalcium) inhibits cholesterol synthesis from acetic acid with an IC50 of 5.8 nM in HepG2 cells. Pitavastatin Calcium inhibits the growth of a panel of ovarian cancer cells, including those considered most likely to represent high-grade serous ovarian cancer (HGSOC), grown as a monolayers (IC50 = 0.4-5 μM) or as spheroids (IC50=0.6-4 μM). 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. Pitavastatin (1 μM, 48 hours) caused PARP cleavage in Ovcar-8 cells. Pitavastatin Calcium (59 mg/kg; p.o.; twice daily for 28 days) caused significant tumour regression [5]. EL mRNA expression was inhibited after treatment with pitavastatin for 6 h, and maximal inhibition occurred and reached plateau after treatment for 24 h. The plasma levels of total cholesterol in mice treated with pitavastatin or vehicle were 2.04+0.15 and 2.18+0.23 mmol/L, respectively(n.s.). The plasma HDL-C levels in mice with or without pitavastatin were 1.87+0.11 and 2.02+0.22 mmol/L, respectively (n.s.). EL expression in vivo through the Rho signalling pathway, and the effect was irrespective of the plasma cholesterol levels[6].
作用机制 Pitavastatin increased the mRNA levels of CYP7A1 in HepG2 cells, suggesting that increased conversion of cholesterol to bile acids may be the mechanism for its potent low-density lipoprotein cholesterol-lowering effects[3].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT03418974 Dyslipidemias Phase 4 Active, not recruiting December 31, 2021 China, Beijing ... 展开 >> Heart Center of Peking University People's Hospital Beijing, Beijing, China, 100044 China, Shanghai School of Public Health, Fudan University Shanghai, Shanghai, China, 200032 收起 <<
NCT01178853 - Completed - -
NCT00242944 Coronary Disease ... 展开 >> Hypercholesterolemia 收起 << Phase 4 Completed - Japan ... 展开 >> Juntendo University School of Medicine Bunkyo-ku, Tokyo, Japan, 113-8421 Yamaguchi University Graduate School of Medicine Ube, Yamaguchi, Japan, 755-8505 Kyoto University Graduate School of Medicine Kyoto, Japan, 606-8507 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.14mL

0.23mL

0.11mL

5.68mL

1.14mL

0.57mL

11.35mL

2.27mL

1.14mL
参考文献

[1]Ahmad H, Cheng-Lai A. Pitavastatin: a new HMG-CoA reductase inhibitor for the treatment of hypercholesterolemia. Cardiol Rev. 2010 Sep-Oct;18(5):264-7.

[2]Maejima T, Yamazaki H, et al. Effect of pitavastatin on apolipoprotein A-I production in HepG2 cell. Biochem Biophys Res Commun. 2004 Nov 12;324(2):835-9.

[3] Ping Fan,et al. Circ J. Pitavastatin, a potent hydroxymethylglutaryl coenzyme a reductase inhibitor, increases cholesterol 7 alpha-hydroxylase gene expression in HepG2 cells2004 Nov;68(11):1061-6.

[4] Igel M, Sudhop T, von Bergmann K. Pharmacology of 3-hydroxy-3-methylglutaryl-coenzyme A reductase inhibitors (statins), including rosuvastatin and pitavastatin. J Clin Pharmacol 2002;42:835-45

[5] Elizabeth de Wolf,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.

[6]Yoko Kojima，et al. Pitavastatin decreases the expression of endothelial lipase both in vitro and in vivo.Cardiovasc Res.2010 Jul 15;87(2):385-93.