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产品名称：BI 224436

产品别名：见爱必信官网

英文别名：BI 224436

靶点：HIV Integrase

CAS：1155419-89-8

纯度：

外观：见爱必信官网

保存方法：

描述：BI 224436 is a novel HIV-1 noncatalytic site integrase inhibitor with EC50 values of less than 15 nM against different HIV-1 laboratory strains.

溶解性：10 mM in DMSO

体外研究：

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 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. 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.

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

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