Pitavastatin (NK-104) 是有效的羟甲基戊二酰-CoA(HMG-CoA)还原酶抑制剂。Pitavastatin 抑制乙酸合成胆固醇，在 HepG2 细胞中的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。Pitavastatin具有抗动脉粥样硬化、抗哮喘、抗骨关节炎、抗肿瘤、神经保护、肝保护和肾保护等作用。

Pitavastatin (NK-104) is a potent hydroxymethylglutaryl-CoA (HMG-CoA) reductase inhibitor. Pitavastatin inhibits cholesterol synthesis from acetic acid with an IC 50 of 5.8 nM in HepG2 cells. Pitavastatin is an efficient hepatocyte low-density lipoprotein-cholesterol (LDL-C) receptor inducer. Pitavastatin process the anti-atherosclerotic, anti-asthmatic, anti-osteoarthritis, antineoplastic, neuroprotective, hepatoprotective and reno-protective effects activity.

Pitavastatin inhibits the growth of a panel of ovarian cancer cells, including those considered most likely to represent HGSOC, grown as a monolayers (IC 50 =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 and caspase-8 and caspase-9 in Ovcar-8 cells and Ovcar-3 cells [4]. Pitavastatin (1 μM, 48 hours) resulted in PARP cleavage in Ovcar-8 cells [4]. Western Blot Analysis [1] Cell Line: Ovcar-8 cells Concentration: 1 μM Incubation Time: 48 hours Result: Induced PARP cleavage.

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

147511-69-1

C25H24FNO4

421.46

Compound T7072

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years