1. Anti-infection
  2. HIV
  3. Temsavir

Temsavir (Synonyms: BMS-626529)

Cat. No.: HY-15440 Purity: 99.46%
Handling Instructions

Temsavir (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.

Temsavir Chemical Structure

Temsavir Chemical Structure

CAS No. : 701213-36-7

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10 mM * 1 mL in DMSO USD 198 In-stock
Estimated Time of Arrival: December 31
5 mg USD 180 In-stock
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10 mg USD 300 In-stock
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50 mg USD 900 In-stock
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100 mg USD 1140 In-stock
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Customer Review

Based on 2 publication(s) in Google Scholar

Other Forms of Temsavir:

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Description

Temsavir (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

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[1]. 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[2].

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

Clinical Trial
Molecular Weight

473.48

Formula

C₂₄H₂₃N₇O₄

CAS No.

701213-36-7

SMILES

O=C(N1CCN(C(C2=CC=CC=C2)=O)CC1)C(C3=CNC4=C3C(OC)=CN=C4N5C=NC(C)=N5)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 16.67 mg/mL (35.21 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent 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.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 1.67 mg/mL (3.53 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 1.67 mg/mL (3.53 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 1.67 mg/mL (3.53 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Kinase Assay
[1]

Micro BioSpin 6 columns are used to measure the binding of [3H]BMS-488043 or [3H]Temsavir 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]Temsavir 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]Temsavir 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]

Cytotoxicity assays are performed in the presence of serially diluted Temsavir 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

Purity: 99.46%

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Keywords:

TemsavirBMS-626529BMS626529BMS 626529HIVHuman immunodeficiency virusInhibitorinhibitorinhibit

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