Free shipping on all orders over $ 500

BMS-626529

Cat. No. M8972
BMS-626529 Structure
Synonym:

Temsavir

Size Price Availability Quantity
5mg USD 157.5  USD175 In stock
10mg USD 252  USD280 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control
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 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.

Chemical Information
Molecular Weight 473.48
Formula C24H23N7O4
CAS Number 701213-36-7
Purity 99.52%
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.

Related HIV Protease Products
Cabotegravir

Cabotegravir, also known as S/GSK1265744 or GSK744, is potent HIV integrase inhibitor.

Tenofovir hydrate

Tenofovir hydrate is a nucleotide reverse transcriptase inhibitor to treat HIV and chronic Hepatitis B.

Diphyllin

Diphyllin is an arylnaphthalene lignan isolated from Justicia procumbens and is a potent HIV-1 inhibitor with an IC50 of 0.38 μM.

Diethyldithiocarbamate sodium

Sodium diethyldithiocarbamate is an accelerator of the rate of copper cementation. Sodium diethyldithiocarbamate reduces the incidence of HIV infection.

Apelin-36(rat, mouse) TFA

Apelin-36(rat, mouse) TFA is an endogenous orphan G protein-coupled receptor APJ agonist.

  Catalog
Abmole Inhibitor Catalog 2017




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

Contact Us

Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2020 AbMole BioScience. All Rights Reserved.