产品
编 号:F171715
分子式:C25H24FNO4
分子量:421.46
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10mM*1mL in DMSO
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5mg
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10mg
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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. Pitavastatin also possesses anti-atherosclerotic, anti-asthmatic, anti-osteoarthritis, antineoplastic, neuroprotective, hepatoprotective and reno-protective effects.

体内研究:
Pitavastatin (59?mg/kg; p.o.; twice daily for 28 days) causes significant tumour regression.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.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.
Animal Model:Female New Zealand white rabbits (diet induced severe hyperlipidemia)
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-.

体外研究:
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).?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.Pitavastatin (1?μM, 48?hours) causes PARP cleavage in Ovcar-8 cells.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.
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