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Lopinavir(ABT-378 Kaletra Aluvia)
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
Lopinavir(ABT-378 Kaletra Aluvia)图片
CAS NO:192725-17-0
规格:≥98%
包装与价格：
包装价格(元)
50mg电议
100mg电议
250mg电议
500mg电议
1g电议
2g电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)628.8
FormulaC37H48N4O5
CAS No.192725-17-0
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 126 mg/mL (200.4 mM)
Water: <1 mg/mL
Ethanol: 126 mg/mL (200.4 mM)
Solubility (In vivo)30% PEG400+0.5% Tween80+5% propylene glycol: 30 mg/mL
SynonymsABT-378; A-157378.0; ABT 378; trade names: Aluviran; Koletra; ABT378; A 157378.0; A157378.0;

Chemical Name: (2S)-N-[(2S,4S,5S)-5-[[2-(2,6-dimethylphenoxy)acetyl]amino]-4-hydroxy-1,6-diphenylhexan-2-yl]-3-methyl-2-(2-oxo-1,3-diazinan-1-yl)butanamide

InChi Key: KJHKTHWMRKYKJE-SUGCFTRWSA-N

InChi Code: InChI=1S/C37H48N4O5/c1-25(2)34(41-20-12-19-38-37(41)45)36(44)39-30(21-28-15-7-5-8-16-28)23-32(42)31(22-29-17-9-6-10-18-29)40-33(43)24-46-35-26(3)13-11-14-27(35)4/h5-11,13-18,25,30-32,34,42H,12,19-24H2,1-4H3,(H,38,45)(H,39,44)(H,40,43)/t30-,31-,32-,34-/m0/s1

SMILES Code: CC1=C(C(=CC=C1)C)OCC(=O)N[C@@H](CC2=CC=CC=C2)[C@H](C[C@H](CC3=CC=CC=C3)NC(=O)[C@H](C(C)C)N4CCCNC4=O)O

实验参考方法
In Vitro

In vitro activity: 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.

Kinase Assay: 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.

Cell Assay: 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.

In VivoLopinavir (10 mg/kg, orally) results in Cmax of 0.8 μg/mL and oral bioavailability of 25% in rats.
Animal modelSprague-Dawley-derived rats or cynomolgus monkeys
Formulation & DosageDissolved in ethanol-propylene glycol-D5W;10 mg/kg; p.o.
ReferencesAntimicrob Agents Chemother. 1998 Dec;42(12):3218-24; Drug Metab Dispos. 1999 Jan;27(1):86-91.
生物活性

Mean ± SD plasma ABT-378 levels in healthy human volunteers following administration of a single 400-mg dose. Dashed line, ABT-378 dosed singly; solid line, ABT-378 dosed with 50 mg of ritonavir; dotted line, EC50 of ABT-378 against wild type (WT) HIV in vitro. Antimicrob Agents Chemother. 1998 Dec;42(12):3218-24.

Inhibition of the metabolism of ABT-378 and saquinavir by ritonavir in rat and human liver microsomes. Antimicrob Agents Chemother. 1998 Dec;42(12):3218-24.

Mean ± standard error of the mean plasma ABT-378 levels after oral dosing with 10 mg/kg singly and in combination with various doses of ritonavir in rats. Antimicrob Agents Chemother. 1998 Dec;42(12):3218-24.