| 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 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.? |
| Synonyms | BMS-663068 Tris |
| molecular weight | 704.62 |
| Molecular formula | C29H37N8O11P |
| CAS | 864953-39-9 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 125 mg/mL (177.40 mM), Sonication is recommended. H2O: 100 mg/mL (141.92 mM), Sonication is recommended. |
| References | 1. Nowicka-Sans B, et al. In vitro antiviral characteristics of HIV-1 attachment inhibitor BMS-626529, the active component of the prodrug BMS-663068. Antimicrob Agents Chemother. 2012 Jul;56(7):3498-507. |