Powder: -20°C for 3 years | In solvent: -80°C for 1 year
BI 224436 is an inhibitor of HIV-1 noncatalytic site integrase. With EC50 values of less than 15 nM against different HIV-1 laboratory strains.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
2 mg | 10-14 weeks | $ 198.00 | |
5 mg | 10-14 weeks | $ 347.00 | |
25 mg | 10-14 weeks | $ 1,140.00 | |
50 mg | 10-14 weeks | $ 1,490.00 | |
100 mg | 10-14 weeks | $ 1,990.00 |
Description | BI 224436 is an inhibitor of HIV-1 noncatalytic site integrase. With EC50 values of less than 15 nM against different HIV-1 laboratory strains. |
Targets&IC50 | HIV-1:(EC50)15 nM |
In vitro | BI 224436 exhibits over 90 μM cellular cytotoxicity and retains its antiviral efficacy with a minimal 2.1-fold reduction in the presence of 50% human serum. It possesses favorable in vitro drug-like absorption, distribution, metabolism, and excretion (ADME) characteristics, such as Caco-2 cell permeability, solubility, and minimal cytochrome P450 inhibition[1]. Moreover, BI 224436 maintains complete antiviral functionality against recombinant viruses bearing integrase strand transfer inhibitor (INSTI) resistance mutations, namely N155S, Q148H, and E92Q. Additionally, it demonstrates an additive effect when used alongside most approved antiretrovirals, including INSTIs. |
In vivo | BI 224436 demonstrates favorable pharmacokinetic properties across multiple species, including rats, monkeys, and dogs. Specifically, in rats, the compound has a clearance rate of 0.7% as a percentage of hepatic flow and a bioavailability of 54%. In monkeys, the clearance rate is 23% with an 82% bioavailability, while in dogs, the clearance is 8%, with bioavailability reaching 81%[1]. |
Molecular Weight | 442.51 |
Formula | C27H26N2O4 |
CAS No. | 1155419-89-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 50 mg/mL (112.99 mM)
You can also refer to dose conversion for different animals. More
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BI 224436 1155419-89-8 Microbiology/Virology Proteases/Proteasome HIV Protease BI224436 BI-224436 inhibitor inhibit