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BMS-626529

Cat. No. M8972
BMS-626529 Structure
Synonym:

Temsavir

Size Price Availability Quantity
5mg USD 120  USD120 In stock
10mg USD 195  USD195 In stock
50mg USD 620  USD620 In stock
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Quality Control & Documentation
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 (for reference only)
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
Chemical Information
Molecular Weight 473.48
Formula C24H23N7O4
CAS Number 701213-36-7
Solubility (25°C) DMSO: 10 mM
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

References

[1] Nettles RE, et al. J Infect Dis. Pharmacodynamics, safety, and pharmacokinetics of BMS-663068, an oral HIV-1 attachment inhibitor in HIV-1-infected subjects.

[2] Nowicka-Sans B, et al. Antimicrob Agents Chemother. In vitro antiviral characteristics of HIV-1 attachment inhibitor BMS-626529, the active component of the prodrug BMS-663068.

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


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