1. Anti-infection
  2. HIV

BMS-626529 (Synonyms: Temsavir)

Cat. No.: HY-15440 Purity: 98.91%
Data Sheet SDS Handling Instructions

BMS-626529 is a novel attachment inhibitor that targets HIV-1 gp120 and prevents its binding to CD4+ T cells.

For research use only. We do not sell to patients.
BMS-626529 Chemical Structure

BMS-626529 Chemical Structure

CAS No. : 701213-36-7

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO $165 In-stock
5 mg $150 In-stock
10 mg $250 In-stock
50 mg $750 In-stock
100 mg $950 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Other Forms of BMS-626529:

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

BMS-626529 is a novel attachment inhibitor that targets HIV-1 gp120 and prevents its binding to CD4+ T cells.

IC50 & Target

HIV-1[1]

In Vitro

BMS-626529 has half-maximal effective concentration (EC50) 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. The cytotoxicity profile of BMS-626529 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 BMS-626529 exhibits low cytotoxicity in cell culture[1]. BMS-626529 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[2].

Clinical Trial
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References
Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 2.1120 mL 10.5601 mL 21.1202 mL
5 mM 0.4224 mL 2.1120 mL 4.2240 mL
10 mM 0.2112 mL 1.0560 mL 2.1120 mL
Please refer to the solubility information to select the appropriate solvent.
Kinase Assay
[1]

Micro BioSpin 6 columns are used to measure the binding of [3H]BMS-488043 or [3H]BMS-626529 to gp120. Binding solutions (30 μL) containing 25 mM Tris-HCl (pH 7.5), 125 mM NaCl, 50 nM gp120JRFL, and serial dilutions of [3H]BMS-488043 or [3H]BMS-626529 are allowed to equilibrate and then adsorbed to a MicroBioSpin 6 column. The column is centrifuged (~14,000 rpm) for 5 min, the eluent is collected, and radioactivity is determined with a scintillation counter. To measure dissociative kinetics, 150 nM [3H]BMS-626529 or 90 nM [3H]BMS-488043 is incubated with 60 nM gp120 at ambient temperature for 1 h to achieve equilibrium binding, and then a large molar excess (14-fold) of soluble CD4 protein is added to drive dissociation. Aliquots are taken at the indicated time intervals, adsorbed to a spin column, and centrifuged, and the radioactivity in the eluent is quantitated. Comparison of the tritium signal from parallel samples with and without the soluble CD4 challenge allowed for the determination of the percent compound bound[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay
[1]

BMS-626529 is dissolved in DMSO and stored, and then diluted with appropriate media before use[1].

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[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

473.48

Formula

C₂₄H₂₃N₇O₄

CAS No.

701213-36-7

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Purity: 98.91%

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Product Name:
BMS-626529
Cat. No.:
HY-15440
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