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。

BI 224436 is a novel HIV-1 noncatalytic site integrase inhibitor with EC 50 values of less than 15 nM against different HIV-1 laboratory strains.

Solid

EC50: 15 nM (HIV-1)

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. has not independently confirmed the accuracy of these methods. They are for reference only.

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%). has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Fenwick C, et al. Preclinical profile of BI 224436, a novel HIV-1 non-catalytic-site integrase inhibitor. Antimicrob Agents Chemother. 2014 Jun;58(6):3233-44.

In Vitro: DMSO : ≥ 50 mg/mL (112.99 mM)配制储备液