| Name | Fostemsavir Tris |
| Description | Fostemsavir Tris (BMS-663068 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. |
| In vivo | 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.?
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| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 125 mg/mL (177.40 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 4 mg/mL (5.68 mM), Sonication is recommended.
H2O : 100 mg/mL (141.92 mM), Sonication is recommended.
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| Keywords | Inhibitor | inhibit | Human immunodeficiency virus | HIVProtease | HIV-1 | HIV Protease | HIV | Fostemsavir Tris | Fostemsavir | BMS-663068 | BMS663068 | BMS 663068 |
| Inhibitors Related | Stavudine | 5-Fluorouracil | Emtricitabine | Kaempferol | Dolutegravir intermediate-1 | Dimethyl fumarate | Lamivudine | Chloroquine phosphate | Valproic Acid | Decanedioic acid | Dextran sulfate sodium salt (MW 5000) | Tenofovir |
| Related Compound Libraries | Target-Focused Phenotypic Screening Library | Bioactive Compound Library | Approved Drug Library | EMA Approved Drug Library | Anti-Viral Compound Library | Drug Repurposing Compound Library | Inhibitor Library | FDA-Approved Drug Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max | Covalent Inhibitor Library | Anti-Infection Compound Library |
United States
