Fostemsavir Tris

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Fostemsavir Tris 是 BMS-626529 的前药，是一种口服、安全、有效的 HIV-1 附着抑制剂。它通过与 gp120 结合并干扰病毒与 CD4+ T 细胞的附着来抑制人类免疫缺陷病毒 1 型 (HIV-1) 感染。

Fostemsavir Tris is the prodrug of BMS-626529,is a oral, safe and effective?inhibitor of HIV-1 attachment.?It inhibits human immunodeficiency virus type 1 (HIV-1) infection by binding to gp120 and interfering with the attachment of virus to CD4+ T-cells.BMS-663068 is the phosphonooxymethyl prodrug of BMS-626529, a novel small-molecule attachment inhibitor that targets HIV-1 gp120 and prevents its binding to CD4(+) T cells.The activity of BMS-626529 is virus dependent, due to heterogeneity within gp120.?BMS-626529 had half-maximal effective concentration (EC(50)) values of <10 nM against the vast majority of viral isolates;?however, susceptibility varied by >6 log(10), with half-maximal effective concentration values in the low pM range against the most susceptible viruses.?The in vitro antiviral activity of BMS-626529 was generally not associated with either tropism or subtype, with few exceptions.?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):Fostemsavir Tris has good antiviral activity in subjects infected with virus shown to be susceptible (IC50, <100 nM) to the agent.

——

Fostemsavir Tris has good antiviral activity in subjects infected with virus shown to be susceptible (IC50, <100 nM) to the agent.

BMS-663068 Tris,FOSTEMSAVIR TROMETHAMINE

Microbiology/Virology

HIV

HIV-1

——

——

864953-39-9

704.62

C29H37N8O11P

>98% (HPLC)

DMSO:125 mg/mL (177.40 mM; Need ultrasonic); H2O:100 mg/mL (141.92 mM; Need ultrasonic)

O=C(N1CCN(C(C2=CC=CC=C2)=O)CC1)C(C3=CN(COP(O)(O)=O)C4=C3C(OC)=CN=C4N5N=C(C)N=C5)=O.OCC(CO)(N)CO

——

(-20℃)

With Ice Pack

≥ 2 years