BI 224436

Research use only, not for human use.

BI 224436 is a potent, specific, noncatalytic site integrase inhibitor (NCINI) of HIV-1 with EC50 of 11-27 nM against different HIV-1 laboratory strains.

BI 224436 is a potent, specific, noncatalytic site integrase inhibitor (NCINI) of HIV-1 with EC50 of 11-27 nM against different HIV-1 laboratory strains, with minimal cellular cytotoxicity; exhibits a low, ～2.1-fold decrease in antiviral potency in the presence of 50% human serum andserum-shifted EC95 values ranging between 22 and 75 nM; also retains full antiviral activity against recombinant viruses encoding INSTI resistance substitutions N155S, Q148H, and E92Q; displays an additive effect in combination with most approved antiretrovirals, including INSTIs.HIV Infection Phase 1 Clinical.

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.

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%).

BI224436

Microbiology/Virology

HIV

HIV

Infection

HIV Infection

1155419-89-8

391.467

C24H25NO4

>98% (HPLC)

DMSO : ≥ 50 mg/mL 112.99 mM

O=C(O)[C@H](C1=C(C2=CC(CCCO3)=C3C=C2)C4=CC=CC=C4N=C1)OC(C)(C)C

(2S)-[4-(3,4-Dihydro-2H-chromen-6-yl)-3-quinolinyl][(2-methyl-2-propanyl)oxy]acetic acid

(-20℃)

With Ice Pack

≥ 2 years