Temsavir

SKU: orb1302670

Description

Temsavir (BMS-626529) is an investigational HIV-1 attachment inhibitor that blocks the gp120 glycoprotein, inhibiting viral entry into host CD4+ T-cells. It is a valuable research tool for studying viral entry mechanisms in vitro and has been evaluated in clinical trials for antiretroviral therapy.

Research Area

Infectious Disease & Virology, Protein Biochemistry

Key Properties

• CAS Number: 701213-36-7
• MW: 473.48
• Purity: 97.33% (May vary between batches)
• Formula: C₂₄H₂₃N₇O₄
• SMILES: COc1cnc(-n2cnc(C)n2)c2[nH]cc(C(=O)C(=O)N3CCN(CC3)C(=O)c3ccccc3)c12
• Target: HIV Protease
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (2.11 mM);DMSO:8.57 mg/mL (18.1 mM)

Bioactivity

• In Vitro:
  Temsavir has half-maximal effective concentration (EC50) values of <10 nM against the vast majority of viral isolates. Temsavir exhibits an average EC50 against LAI virus of 0.7±0.4 nM. Temsavir exhibits an EC50 of 0.01 nM against the most susceptible virus and an EC50 of >2,000 nM against the least susceptible virus. The cytotoxicity profile of Temsavir is examined in several cell types from different human tissues. CC50 values of >200 μM are observed in MT-2 (T lymphocytes), HEK293 (kidney), HEp-2 (larynx), HepG2 (liver), HeLa (cervix), HCT116 (colorectal), MCF-7 (breast), SK-N-MC (neuroepithelium), HOS (bone), H292 (lung), and MDBK (bovine kidney) cells measured after 3 or 6 days in culture. CC50 values of 105 and 192 μM are obtained in the T-cell line PM1 and in PBMCs, respectively, following 6 days in culture. These results show that Temsavir exhibits low cytotoxicity in cell culture. Temsavir exhibits a broad spectrum of antiviral activity against a panel of clinical isolates, with a 50% inhibitory concentration (IC50) ranging from subnanomolar levels to >0.1 μM.
• Cell Research:
  Cytotoxicity assays are performed in the presence of serially diluted BMS-626529 for up to 6 days, and cell viability is quantitated using an XTT assay. To determine CC50 values (concentration of drug required to kill 50% of cells), laboratory-adapted peripheral blood mononuclear cells (PBMCs) are initially plated at a density of 0.1×106 cells/mL. In the absence of compounds, the cell densities typically reach 1×106 to 1.2×106/mL after 6 days.

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Temsavir, inhibit, Inhibitor, Human immunodeficiency virus, HIV, HIV Protease, HIVProtease, BMS 626529, BMS626529, BMS-626529

Compound Identifiers

PubChem CID

11317439