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Lopinavir
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图片
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
50mg电议
100mg电议
250mg电议

产品介绍
Lopinavir是一种有效的HIV protease抑制剂,无细胞试验中Ki为1.3 pM。

Cell lines

MT4 cells

Preparation method

The solubility of this compound in DMSO is > 31.5 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 ℃ for several months.

Reacting condition

4 ~ 52 nM

Applications

HIV with multiple mutations was markedly less resistant to Lopinavir than to Ritonavir. Although the activity of Lopinavir declined significantly against the multiply mutated strains compared with its activity against the baseline strains, the extent of the decline was substantially less than that of Ritonavir. Furthermore, the EC50 value of Lopinavir against HIV with multiple mutations was 10-fold lower than that of Ritonavir.

Animal models

Rats

Dosage form

10 mg/kg; p.o.

Applications

The Cmax and oral bioavailability of Lopinavir in rats were 0.8 μg/mL and 25%, respectively. At 6th hr, the plasma level of Lopinavir declined below the level of quantitation (0.01 μg/mL). However, co-administration of Lopinavir with Ritonavir (10 mg/kg) maintained the concentrations of Lopinavir in excess of 3 μg/mL with low variability. In addition, the area under the plasma concentration-time curve from 0 ~ 8 hrs for Lopinavir increased 14-fold due to Ritonavir co-administration.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

产品描述

Lopinavir (also known as ABT-378) is a highly potent inhibitor of human immunodeficiency virus (HIV) protease that potently inhibits wild-type and mutant HIV protease with inhibition constantKivalues ranging from 1.3 to 3.6 pM. Lopinavir, a ritonavir analog designed to have a diminished interaction with Val82 in HIV protease, maintains a high potency inhibiting Val82 mutant HIV selected by ritonavir with 50% effective concentration EC50value lower than 0.06 μM. Although the antiviral activity of ritonavir is considerably attenuated by human serum, lopinavir is less affected by human serum proteins and is 10-fold greater in potency than ritonavir in the presence of human serum.

Reference

[1].Sham HL, Kempf DJ, Molla A, Marsh KC, Kumar GN, Chen CM, Kati W, Stewart K, Lal R, Hsu A, Betebenner D, Korneyeva M, Vasavanonda S, McDonald E, Saldivar A, Wideburg N, Chen X, Niu P, Park C, Jayanti V, Grabowski B, Granneman GR, Sun E, Japour AJ, Leonard JM, Plattner JJ, Norbeck DW. ABT-378, a highly potent inhibitor of the human immunodeficiency virus protease. Antimicrob Agents Chemother. 1998 Dec;42(12):3218-24.