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BI 224436
本半岛bd体育手机客户端 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。
BI 224436图片
CAS NO:1155419-89-8
包装与价格:
包装价格(元)
50 mg电议
100 mg电议

半岛bd体育手机客户端 介绍

半岛bd体育手机客户端 描述

BI 224436 is an inhibitor of HIV-1 noncatalytic site integrase. With EC50 values of less than 15 nM against different HIV-1 laboratory strains.

体外活性

BI 224436 has cellular cytotoxicity of more than 90 μM. BI 224436 has a low, 2.1-fold decrease in antiviral potency in the presence of 50% human serum. BI 224436 has drug-like in vitro absorption, distribution, metabolism, and excretion (ADME) properties, including Caco-2 cell permeability, solubility, and low cytochrome P450 inhibition[1]. BI 224436 retains full antiviral activity against recombinant viruses encoding INSTI resistance substitutions N155S, Q148H, and E92Q. BI 224436 displays an additive effect in combination with most approved antiretrovirals, including INSTIs.

体内活性

BI 224436 exhibits excellent pharmacokinetic profiles in rat (clearance as a percentage of hepatic flow [CL], 0.7%; bioavailability [F], 54%), monkey (CL, 23%; F, 82%), and dog (CL, 8%; F, 81%)[1].

Cas No.

1155419-89-8

分子式

C27H26N2O4

分子量

442.51

别名

BI 224436

储存和溶解度

DMSO:50 mg/mL (112.99 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years
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