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CAS No. : 1155419-89-8
MCE 国际站:BI 224436
产品活性:BI 224436是一种新型的HIV-1非催化性位点整合酶抑制剂,对HIV-1实验室菌株的EC50值小于15 nM。
研究领域:Anti-infection | Metabolic Enzyme/Protease
作用靶点:HIV | HIV Integrase
In Vitro: 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.
In Vivo: 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%).
相关产品:Clinical Compound Library Plus | Bioactive Compound Library Plus | Peldesine dihydrochloride | Abacavir sulfate | HIV-IN-6 | Epicoccone B | Ditiocarb | Nevirapine | DAPTA | Aloperine | Elipovimab | HIV-1 inhibitor-52 | PMEDAP | Integracin B | FNC-TP | DDX3-IN-1 | Sennoside A | CK-666 | HIV-1 inhibitor-44 | Flavopiridol | Claficapavir | Atazanavir | 1-Deoxymannojirimycin hydrochloride | TC14012 | (Z)-9-Propenyladenine | Apabetalone | CCR5 antagonist 2 | 2F5 epitope | HIV-1 inhibitor-23 | Apelin-36(rat, mouse) | MIV-150 | Tenofovir alafenamide hemifumarate
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