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BMS-626529
Cat No.
CEI-1254
Description
BMS-626529 is a small-molecule attachment inhibitor of HIV-1 gp120with IC50 values of 2.26 nM, 0.34 nM and 1.3 nM for HIV-1 subtype A, B, and C envelope, respectively.
Product Overview
EC50 HIV-1 attachment inhibitors represent a new class of entry inhibitors that prevent the initial interaction between virus and host cell by binding to the viral envelope protein gp120 and blocking attachment of the virus to the CD4 receptor on CD4+ T-cells. BMS-626529 is a novel small-molecule attachment inhibitor that targets HIV-1 gp120 and prevents its binding to CD4+ T-cells. Clinical trial: BMS-663068 is a prodrug of the small-molecule inhibitor BMS-626529.The maximum median decreased in plasma HIV-1 RNA load from baseline ranged from 1.21 to 1.73 log10 copies/mL. Plasma concentrations of BMS-626529 were not associated with an antiviral response, while low baseline inhibitory concentrations and the minimum and average steady-state BMS-626529 plasma concentrations, when adjusted by the baseline protein binding-adjusted 90% inhibitory concentration, were linked with antiviral response. BMS-663068 was generally well tolerated.
CAS No.
701213-36-7
Molecular Weight
473.48
Purity
0.9853
Storage
Store at -20°C
Synonyms
BMS 626529; BMS626529
Targets
HIV-1
IC50
2.26 nM; 0.34 nM; 1.3 nM
Molecular Formula
C24H23N7O4
Chemical Name
1-(4-benzoylpiperazin-1-yl)-2-[4-methoxy-7-(3-methyl-1,2,4-triazol-1-yl)-1H-pyrrolo[2,3-c]pyridin-3-yl]ethane-1,2-dione
Solubility
Soluble in DMSO
Shipping Conditions
Evaluation sample solution: ship with blue ice. All other available size: ship with RT, or blue ice upon request
In vitro
The activity of BMS-626529 is virus dependent, due to heterogeneity within gp120. BMS-626529 had half-maximal effective concentration values of6 log10, with half-maximal effective concentration values in the low pM range against the most susceptible viruses. Measurement of the binding affinity of BMS-626529 for purified gp120 suggests that a contributory factor to its inhibitory potency may be a relatively long dissociative half-life.
In vivo
No animal in-vivo data available currently
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