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。Pitavastatin 还具有抗动脉粥样硬化、抗哮喘、抗骨关节炎、抗肿瘤、神经保护、肝保护和肾保护作用。
| 生物活性 | Pitavastatin (NK-104) is a potenthydroxymethylglutaryl-CoA (HMG-CoA) reductaseinhibitor. Pitavastatin inhibitscholesterolsynthesis from acetic acid with anIC50of 5.8 nM in HepG2 cells. Pitavastatin is an efficient hepatocyte low-density lipoprotein-cholesterol (LDL-C) receptor inducer. Pitavastatin also possesses anti-atherosclerotic, anti-asthmatic, anti-osteoarthritis, antineoplastic, neuroprotective, hepatoprotective and reno-protective effects[1][2][3][8]. |
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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) causes PARP cleavage in Ovcar-8 cells[4].
Pitavastatin (0.1 and 1 μM; 1 h, then cells incubate with TNF-α for 6 h) increases the expression of ICAM-1 mRNA through suppressing NF-κB pathway in TNF-α-stimulated human saphenous vein endothelial cells[6].
Western Blot Analysis[4] | Cell Line: | Ovcar-8 cells | | Concentration: | 1 μM | | Incubation Time: | 48 hours | | Result: | Induced PARP cleavage. |
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体内研究
(In Vivo) | Pitavastatin (59 mg/kg; p.o.; twice daily for 28 days) causes significant tumour regression[4].
Pitavastatin (0.1 mg/kg; p.o; daily for 12 weeks) retards the progression of atherosclerosis formation and improves NO bioavailability by eNOS up-regulation and decrease of O2-in diet induced severe hyperlipidemia rabbit model[7].
| 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. |
| Animal Model: | Female New Zealand white rabbits (diet induced severe hyperlipidemia)[7] | | Dosage: | 0.1 mg/kg | | Administration: | p.o; daily for 12 weeks | | Result: | Retarded the progression of atherosclerosis formation and improved NO bioavailability by eNOS up-regulation and decrease of O2-. |
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| 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. |
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