BMS-378806

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Chemical Information

Product name：BMS-378806	Purity：98% min
CAS NO：357263-13-9	Solubility：DMSO : ≥ 50 mg/mL (123.02 mM)
Molecular Formula：C₂₂H₂₂N₄O₄	Package：Package according to customer requirements
Molecular Weight：406.434	Storage：Store at -20℃

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Remarks

BMS-378806 is a small molecule that inhibits the first step of HIV-1 infection by blocking the binding of host cell CD4 with viral gp120 protein. It binds the exterior envelope glycoprotein gp120 (Kd= 21.1 nM; Ki = 24.9 nM), blocking the conformational change that occurs with CD4 binding and preventing fusion of the viral and target cell membranes.

References

[1]. Wang T, et al. Discovery of 4-benzoyl-1-[(4-methoxy-1H- pyrrolo[2,3-b]pyridin-3-yl)oxoacetyl]-2- (R)-methylpiperazine (BMS-378806): a novel HIV-1 attachment inhibitor that interferes with CD4-gp120 interactions. J Med Chem. 2003 Sep 25;46(20):4236-9.

[2]. Ho HT, et al. Envelope conformational changes induced by human immunodeficiency virus type 1 attachment inhibitors prevent CD4 binding and downstream entry events. J Virol. 2006 Apr;80(8):4017-25.