| CAS NO: | 192725-17-0 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 50mg | 电议 |
| 100mg | 电议 |
| 250mg | 电议 |
| 500mg | 电议 |
| 1g | 电议 |
| 2g | 电议 |
| Molecular Weight (MW) | 628.8 |
|---|---|
| Formula | C37H48N4O5 |
| 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 |
| Synonyms | ABT-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 |
| 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 Vivo | Lopinavir (10 mg/kg, orally) results in Cmax of 0.8 μg/mL and oral bioavailability of 25% in rats. |
| Animal model | Sprague-Dawley-derived rats or cynomolgus monkeys |
| Formulation & Dosage | Dissolved in ethanol-propylene glycol-D5W;10 mg/kg; p.o. |
| References | Antimicrob Agents Chemother. 1998 Dec;42(12):3218-24; Drug Metab Dispos. 1999 Jan;27(1):86-91. |
 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. |  |  |
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