BI 224436CAS号： 1155419-89-8分子式： C27H26N2O4分子量： 442.51描述纯度储存/保存方法注意事项可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)
| 产品描述 | |
| 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.
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| 纯度 |
98%
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| 储存/保存方法 |
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
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| 注意事项 |
该产品在溶液状态不稳定，建议您现用现配，即刻使用。
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| 基本信息 | |
| 可溶性/溶解性 |
DMSO : ≥ 50 mg/mL (112.99 mM)
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| 生物活性 | |
| 靶点 |
HIV Integrase
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| In vitro(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 JPorption, distribution, metabolism, and excretion (ADME) properties, including Caco-2 cell permeability, solubility, and low cytochrome P450 inhibition.
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| In vivo(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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分子结构图
