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抑制剂描述:

产品名称:Lopinavir

产品别名:见爱必信官网

英文别名:Lopinavir

靶点:HIV Protease

CAS:192725-17-0

纯度:>98%

外观:见爱必信官网

保存方法:Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.

描述:

Lopinavir是一种有效的HIV protease(HIV蛋白酶)抑制剂, K_i为1.3 pM。Lopinavir与突变型 HIV 蛋白酶(V82A, V82F 和 V82T)结合,K_i分别为4.9 pM, 3.7 pM和 3.6 pM。0.5 nM Lopinavir抑制93%野生型HIV蛋白酶活性。Lopinavir作用于MT4细胞,在有或无50% HS存在时,Lopinavir抑制HIV蛋白酶活性,EC50 分别为 102 nM 和17 nM。

溶解性:Ethanol :116 mg/mL (184.5 mM);
DMSO :116 mg/mL (184.5 mM)

体外研究:

Lopinavir binds to mutant HIV protease (V82A, V82F and V82T) with Ki of 4.9 pM, 3.7 pM and 3.6 pM, respectively. Lopinavir inhibits 93% of wild-type HIV protease activity at 0.5 nM. Lopinavir inhibits HIV protease activity in the absence and presence of 50% HS with EC50 of 17 nM and 102 nM, respectively, in MT4 cells. Lopinavir is converted to several metabolites in an NADPH-dependent manner in liver microsomes with the primary metabolites M-3 and M-4. Lopinavir is a potent inhibitor of Rh123 efflux in Caco-2 monolayers with IC50 of 1.7 mM. Lopinavir exposure (72 hours) in LS 180V cells reduces the content of intracellular Rh123. Lopinavir induces P-glycoprotein immunoreactive protein and messenger RNA levels in LS 180V cells. Lopinavir inhibits subtype C clone C6 with IC50 of 9.4 nM. Lopinavir inhibits CYP3A with IC50 of 7.3 mM in human liver microsomes, while produces negligible or weak inhibition of human CYP1A2, 2B6, 2C9, 2C19 and 2D6.

体内研究:Lopinavir (10 mg/kg, orally) results in Cmax of 0.8 μg/mL and oral bioavailability of 25% in rats.

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