Art. -Nr.: HY-15440

Temsavir

(Synonyms: BMS-626529)

6 Cited Publications

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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.

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Reinheit: 98.70%
CAS. Nr.: 701213-36-7
Formel: C₂₄H₂₃N₇O₄
Molecular Weight:473.48

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Temsavir Chemical Structure

CAS. Nr.: 701213-36-7

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Clinical Trial
Chemical Information
Publications (6)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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

Alle HIV Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
HCT-116	CC₅₀	>200 μM Compound: 31; BMS-626529	Cytotoxicity against human HCT116 cells after 6 days by XTT assay Cytotoxicity against human HCT116 cells after 6 days by XTT assay	[PMID: 29271653]
HEK293	CC₅₀	>200 μM Compound: 31; BMS-626529	Cytotoxicity against HEK293 cells after 6 days by XTT assay Cytotoxicity against HEK293 cells after 6 days by XTT assay	[PMID: 29271653]
HeLa	CC₅₀	>200 μM Compound: 31; BMS-626529	Cytotoxicity against human HeLa cells after 6 days by XTT assay Cytotoxicity against human HeLa cells after 6 days by XTT assay	[PMID: 29271653]
HeLa	CC₅₀	>300 μM Compound: 1; BMS-626529	Cytotoxicity against human HeLa cells after 6 days by MTT assay Cytotoxicity against human HeLa cells after 6 days by MTT assay	[PMID: 26584882]
HEp-2	CC₅₀	>200 μM Compound: 31; BMS-626529	Cytotoxicity against human Hep2 cells after 6 days by XTT assay Cytotoxicity against human Hep2 cells after 6 days by XTT assay	[PMID: 29271653]
HepG2	CC₅₀	>200 μM Compound: 31; BMS-626529	Cytotoxicity against human HepG2 cells after 6 days by XTT assay Cytotoxicity against human HepG2 cells after 6 days by XTT assay	[PMID: 29271653]
HOS	CC₅₀	>200 μM Compound: 31; BMS-626529	Cytotoxicity against HOS cells after 6 days by XTT assay Cytotoxicity against HOS cells after 6 days by XTT assay	[PMID: 29271653]
MCF7	CC₅₀	>200 μM Compound: 31; BMS-626529	Cytotoxicity against human MCF7 cells after 6 days by XTT assay Cytotoxicity against human MCF7 cells after 6 days by XTT assay	[PMID: 29271653]
MT2	CC₅₀	>200 μM Compound: 31; BMS-626529	Cytotoxicity against human MT2 cells after 6 days by XTT assay Cytotoxicity against human MT2 cells after 6 days by XTT assay	[PMID: 29271653]
MT2	CC₅₀	>300 μM Compound: 3; BMS-626529	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	[PMID: 29920093]
MT2	CC₅₀	>300 μM Compound: 3	Cytotoxicity against human MT2 cells assessed as decrease in cell viability Cytotoxicity against human MT2 cells assessed as decrease in cell viability	[PMID: 30940396]
MT2	EC₅₀	0.7 nM Compound: 12a	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	[PMID: 26116177]
MT2	EC₅₀	14.8 nM Compound: 12a	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	[PMID: 26116177]
MT2	EC₅₀	16.2 nM Compound: 12a	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	[PMID: 26116177]
MT2	EC₅₀	2.2 nM Compound: 12a	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	[PMID: 26116177]
NCI-H292	CC₅₀	>200 μM Compound: 31; BMS-626529	Cytotoxicity against human NCI-H292 cells after 6 days by XTT assay Cytotoxicity against human NCI-H292 cells after 6 days by XTT assay	[PMID: 29271653]
PBMC	CC₅₀	>10 μM Compound: BMS-626529	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	[PMID: 29860061]
PBMC	CC₅₀	192 μM Compound: 31; BMS-626529	Cytotoxicity against human PBMC after 6 days by XTT assay Cytotoxicity against human PBMC after 6 days by XTT assay	[PMID: 29271653]
SK-N-MC	CC₅₀	>200 μM Compound: 31; BMS-626529	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	[PMID: 29271653]
TZM	CC₅₀	>100 μM Compound: BMS-626529	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	[PMID: 32031803]

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].

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

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 701213-36-7
Appearance Solid
Molecular Weight 473.48
Formel C₂₄H₂₃N₇O₄
SMILES

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

BMS-626529
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

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

Lösungsmittel & Löslichkeit

In Vitro:

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.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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. 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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 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

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.

Protocol 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

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

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

This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Protokoll

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 gp120_JRFL, 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.

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].

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (285 KB)
SDS (583 KB)
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COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

Temsavir

6 Cited Publications

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Temsavir

Bioactive Compound Library Max

Bioactive Compound Library

Anti-Infection Compound Library

Clinical Compound Library

Antiviral Compound Library

Peptidomimetic Library

Covalent Screening Library

Human Metabolite Library

MCE Bioactive Compound Library

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High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Publications Citing Use of MedChemExpress (MCE) Temsavir

Alle HIV Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (6)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Temsavir

Bioactive Compound Library Max

Bioactive Compound Library

Anti-Infection Compound Library

Clinical Compound Library

Antiviral Compound Library

Peptidomimetic Library

Covalent Screening Library

Human Metabolite Library

MCE Bioactive Compound Library

Covalent Screening Library Plus

Clinical Compound Library Plus

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Publications Citing Use of MedChemExpress (MCE) Temsavir

Alle HIV Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (6)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Temsavir Related Classifications

HY-15440 Related Classifications