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BMS-626529

Cat. No. M8972
BMS-626529 Structure
Synonym:

Temsavir

Size Price Availability Quantity
5mg USD 175 In stock
10mg USD 280 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

BMS-626529 (Temsavir) is a potent HIV-1 attachment inhibitor that targets HIV-1 gp120 and prevents its binding to CD4(+) T cells. BMS-626529 had half-maximal effective concentration (EC(50)) values of <10 nM against the vast majority of viral isolates. BMS-626529 exhibits an average EC50 against LAI virus of 0.7±0.4 nM. BMS-626529 exhibits an EC50 of 0.01 nM against the most susceptible virus and an EC50 of >2,000 nM against the least susceptible virus. BMS-626529 exhibits a broad spectrum of antiviral activity against a panel of clinical isolates, with an IC50 ranging from subnanomolar levels to >0.1 µM.

Protocol
Cell Experiment
Cell lines PBMCs
Preparation method 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.
Concentrations
Incubation time 6 days
Animal Experiment
Animal models
Formulation
Dosages
Administration
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 473.48
Formula C24H23N7O4
CAS Number 701213-36-7
Purity >98%
Solubility DMSO: 10 mM
Storage at -20°C
References

Pharmacodynamics, safety, and pharmacokinetics of BMS-663068, an oral HIV-1 attachment inhibitor in HIV-1-infected subjects.
Nettles RE, et al. J Infect Dis. 2012 Oct 1;206(7):1002-11. PMID: 22896665.

In vitro antiviral characteristics of HIV-1 attachment inhibitor BMS-626529, the active component of the prodrug BMS-663068.
Nowicka-Sans B, et al. Antimicrob Agents Chemother. 2012 Jul;56(7):3498-507. PMID: 22547625.

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Keywords: BMS-626529, Temsavir supplier, HIV Protease, inhibitors

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