Temsavir
Based on 6 publication(s) in Google Scholar
Temsavir (BMS-626529) is a novel attachment inhibitor that targets HIV-1 gp120 and prevents its binding to CD4+ T cells.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 98.70%
- CAS No.: 701213-36-7
- Formule: C24H23N7O4
- Masse moléculaire:473.48
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Temsavir
More- Commun Biol. 2021 Jan 20;4(1):93. [Abstract]
- Molecules. 2020 Mar 21;25(6):1430. [Abstract]
- J Antimicrob Chemother. 2021 Nov 12;76(12):3310-3312. [Abstract]
- J Antimicrob Chemother. 2020 Sep 1;75(9):2547-2553. [Abstract]
- J Chromatogr B Analyt Technol Biomed Life Sci. 2025 Dec 15:1267:124803. [Abstract]
- bioRxiv. 2025 Dec 27:2025.12.27.696684. [Abstract]
Activité biologique
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HIV-1 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HCT-116 | CC50 |
>200 μM
Compound: 31; BMS-626529
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Cytotoxicity against human HCT116 cells after 6 days by XTT assay
Cytotoxicity against human HCT116 cells after 6 days by XTT assay
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[PMID: 29271653] |
| HEK293 | CC50 |
>200 μM
Compound: 31; BMS-626529
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Cytotoxicity against HEK293 cells after 6 days by XTT assay
Cytotoxicity against HEK293 cells after 6 days by XTT assay
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[PMID: 29271653] |
| HeLa | CC50 |
>200 μM
Compound: 31; BMS-626529
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Cytotoxicity against human HeLa cells after 6 days by XTT assay
Cytotoxicity against human HeLa cells after 6 days by XTT assay
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[PMID: 29271653] |
| HeLa | CC50 |
>300 μM
Compound: 1; BMS-626529
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Cytotoxicity against human HeLa cells after 6 days by MTT assay
Cytotoxicity against human HeLa cells after 6 days by MTT assay
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[PMID: 26584882] |
| HEp-2 | CC50 |
>200 μM
Compound: 31; BMS-626529
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Cytotoxicity against human Hep2 cells after 6 days by XTT assay
Cytotoxicity against human Hep2 cells after 6 days by XTT assay
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[PMID: 29271653] |
| HepG2 | CC50 |
>200 μM
Compound: 31; BMS-626529
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Cytotoxicity against human HepG2 cells after 6 days by XTT assay
Cytotoxicity against human HepG2 cells after 6 days by XTT assay
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[PMID: 29271653] |
| HOS | CC50 |
>200 μM
Compound: 31; BMS-626529
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Cytotoxicity against HOS cells after 6 days by XTT assay
Cytotoxicity against HOS cells after 6 days by XTT assay
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[PMID: 29271653] |
| MCF7 | CC50 |
>200 μM
Compound: 31; BMS-626529
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Cytotoxicity against human MCF7 cells after 6 days by XTT assay
Cytotoxicity against human MCF7 cells after 6 days by XTT assay
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[PMID: 29271653] |
| MT2 | CC50 |
>200 μM
Compound: 31; BMS-626529
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Cytotoxicity against human MT2 cells after 6 days by XTT assay
Cytotoxicity against human MT2 cells after 6 days by XTT assay
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[PMID: 29271653] |
| MT2 | CC50 |
>300 μM
Compound: 3; BMS-626529
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Cytotoxicity against human MT2 cells assessed as decrease in cell viability after 3 days by XTT assay
Cytotoxicity against human MT2 cells assessed as decrease in cell viability after 3 days by XTT assay
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[PMID: 29920093] |
| MT2 | CC50 |
>300 μM
Compound: 3
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Cytotoxicity against human MT2 cells assessed as decrease in cell viability
Cytotoxicity against human MT2 cells assessed as decrease in cell viability
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[PMID: 30940396] |
| MT2 | EC50 |
0.7 nM
Compound: 12a
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Antiviral activity against CXCR4-tropic HIV1 LAI infected in human MT2 cells by monogram phenosense entry assay
Antiviral activity against CXCR4-tropic HIV1 LAI infected in human MT2 cells by monogram phenosense entry assay
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[PMID: 26116177] |
| MT2 | EC50 |
14.8 nM
Compound: 12a
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Antiviral activity against CXCR4-tropic HIV1 MN infected in human MT2 cells by monogram phenosense entry assay
Antiviral activity against CXCR4-tropic HIV1 MN infected in human MT2 cells by monogram phenosense entry assay
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[PMID: 26116177] |
| MT2 | EC50 |
16.2 nM
Compound: 12a
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Antiviral activity against CXCR4-tropic HIV1 3B infected in human MT2 cells by monogram phenosense entry assay
Antiviral activity against CXCR4-tropic HIV1 3B infected in human MT2 cells by monogram phenosense entry assay
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[PMID: 26116177] |
| MT2 | EC50 |
2.2 nM
Compound: 12a
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Antiviral activity against CXCR4-tropic HIV1 NL4-3 infected in human MT2 cells by monogram phenosense entry assay
Antiviral activity against CXCR4-tropic HIV1 NL4-3 infected in human MT2 cells by monogram phenosense entry assay
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[PMID: 26116177] |
| NCI-H292 | CC50 |
>200 μM
Compound: 31; BMS-626529
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Cytotoxicity against human NCI-H292 cells after 6 days by XTT assay
Cytotoxicity against human NCI-H292 cells after 6 days by XTT assay
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[PMID: 29271653] |
| PBMC | CC50 |
>10 μM
Compound: BMS-626529
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Cytotoxicity against human PBMC cells assessed as reduction in cell viability incubated for 1 hr followed by complete medium addition and measured after 48 hrs by XTT assay
Cytotoxicity against human PBMC cells assessed as reduction in cell viability incubated for 1 hr followed by complete medium addition and measured after 48 hrs by XTT assay
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[PMID: 29860061] |
| PBMC | CC50 |
192 μM
Compound: 31; BMS-626529
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Cytotoxicity against human PBMC after 6 days by XTT assay
Cytotoxicity against human PBMC after 6 days by XTT assay
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[PMID: 29271653] |
| SK-N-MC | CC50 |
>200 μM
Compound: 31; BMS-626529
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Cytotoxicity against human SK-N-MC cells after 6 days by XTT assay
Cytotoxicity against human SK-N-MC cells after 6 days by XTT assay
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[PMID: 29271653] |
| TZM | CC50 |
>100 μM
Compound: BMS-626529
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Cytotoxicity against human TZM-bl cells incubated for 3 days by MTS assay
Cytotoxicity against human TZM-bl cells incubated for 3 days by MTS assay
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[PMID: 32031803] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 701213-36-7
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Appearance Solid
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Masse moléculaire 473.48
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Formule C24H23N7O4
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SMILES
O=C(N1CCN(C(C2=CC=CC=C2)=O)CC1)C(C3=CNC4=C3C(OC)=CN=C4N5C=NC(C)=N5)=O
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Synonyms
BMS-626529
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (6)
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Journal Impact Factor
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Most Recent
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Commun Biol
Identification of 3-chymotrypsin like protease (3CLPro) inhibitors as potential anti-SARS-CoV-2 agents. [Abstract]2021 Jan 20;4(1):93. PMID: 33473151 -
Molecules
Composition and Orientation of the Core Region of Novel HIV-1 Entry Inhibitors Influences Metabolic Stability. [Abstract]2020 Mar 21;25(6):1430. PMID: 32245167 -
J Antimicrob Chemother
In vitro susceptibility of HIV-1 CRF02_AG to temsavir, the active compound of the attachment inhibitor fostemsavir. [Abstract]2021 Nov 12;76(12):3310-3312. PMID: 34402509 -
J Antimicrob Chemother
In vitro susceptibility to fostemsavir is not affected by long-term exposure to antiviral therapy in MDR HIV-1-infected patients. [Abstract]2020 Sep 1;75(9):2547-2553. PMID: 32464638 -
J Chromatogr B Analyt Technol Biomed Life Sci
Development, validation and clinical implementation of a HPLC-MS/MS method for the simultaneous quantification of bictegravir, emtricitabine, doravirine, cabotegravir, lenacapavir, fostemsavir, tenofovir alafenamide and the corresponding metabolites temsavir and tenofovir, in human plasma. [Abstract]2025 Dec 15:1267:124803. PMID: 41072339 -
bioRxiv
Comprehensive Mapping of the Virus and Host Factors that Guide the Paths of HIV-1 Escape from a Therapeutic. [Abstract]2025 Dec 27:2025.12.27.696684. PMID: 41497656
Solvant et solubilité
DMSO : ≥ 16.67 mg/mL (35.21 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
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
This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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
This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocole
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureté et documentation
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Fiche technique (285 KB)
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SDS (583 KB)
- English - EN (583 KB)
- Français - FR (583 KB)
- Deutsch - DE (583 KB)
- Norwegian - NO (583 KB)
- Español - ES (583 KB)
- Swedish - SV (583 KB)
- Italian - IT (583 KB)
- Korean - KR (583 KB)
- Portuguese - PT (583 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Nowicka-Sans B, et al. In vitro antiviral characteristics of HIV-1 attachment inhibitor BMS-626529, the active component of the prodrug BMS-663068. Antimicrobial Agents and Chemotherapy (2012), 56(7), 3498-3507. [Content Brief]
[2]. Nettles RE, et al. Pharmacodynamics, safety, and pharmacokinetics of BMS-663068, an oral HIV-1 attachment inhibitor in HIV-1-infected subjects. J Infect Dis. 2012 Oct 1;206(7):1002-11. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.1120 mL | 10.5601 mL | 21.1202 mL | 52.8005 mL |
| 5 mM | 0.4224 mL | 2.1120 mL | 4.2240 mL | 10.5601 mL | |
| 10 mM | 0.2112 mL | 1.0560 mL | 2.1120 mL | 5.2801 mL | |
| 15 mM | 0.1408 mL | 0.7040 mL | 1.4080 mL | 3.5200 mL | |
| 20 mM | 0.1056 mL | 0.5280 mL | 1.0560 mL | 2.6400 mL | |
| 25 mM | 0.0845 mL | 0.4224 mL | 0.8448 mL | 2.1120 mL | |
| 30 mM | 0.0704 mL | 0.3520 mL | 0.7040 mL | 1.7600 mL |
Temsavir Related Classifications
HY-15440 Related Classifications
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