Lopinavir

CAS NO.:192725-17-0

Molecular Formula:C₃₇H₄₈N₄O₅

Molecular Weight:628.8

Purity: > 98%

Solubility (R.T.: 25℃): DMSO

Stability: - 20℃ 2 years

Lopinavir is a potent HIV protease inhibitor with Ki of 1.3 pM. Target: HIV protease 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. Lopinavir (10 mg/kg, orally) results in Cmax of 0.8 μg/mL and oral bioavailability of 25% in rats.

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