Fostemsavir Tris

Research use only, not for human use.

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.

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.

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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

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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

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(-20℃)

With Ice Pack

≥ 2 years