Pitavastatin calcium

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

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 is a novel member of the medication class of statins. The statins are a family of compounds that inhibit 3-hydroxy-3-methyl glutaryl coenzyme A (HMG-CoA) reductase, a pivotal enzyme in cholesterol biosynthesis. Pitavastatin is a potent inhibitor of HMG-CoA reductase (Ki = 1.7 nM). It lowers both total cholesterol and low density lipoprotein cholesterol in animals and humans. Metabolism of pitavastatin by the cytochrome P450 system is minimal, reducing the risk of drug-drug interactions. Moreover, pitavastatin causes atherosclerosis regression in humans with subclinical carotid atherosclerosis and improves cardiac function and survival in a rat model of hypertensive heart failure.(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).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) causes PARP cleavage in Ovcar-8 cells.(In Vivo):Pitavastatin Calcium (59?mg/kg; p.o.; twice daily for 28 days) causes significant tumour regression.

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

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

Itabastatin | Itavastatin | NK 104

Others

Other Targets

cholesterol esters

Cancer

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147526-32-7

880.98

C50H46CaF2N2O8

>98% (HPLC)

DMSO: 51 mg/mL (57.89 mM)

C1C(C1)C2=NC3=CC=CC=C3C(=C2/C=C/[C@@H](O)C[C@@H](O)CC(=O)[O-])C4=CC=C(C=C4)F.C1C(C1)C2=NC3=CC=CC=C3C(=C2/C=C/[C@@H](O)C[C@@H](O)CC(=O)[O-])C4=CC=C(C=C4)F.[Ca+2]

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(-20℃)

With Ice Pack

≥ 2 years