Fig. 1 · Structure

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Temsavir (BMS 626529)

Cat. No. A14148 CAS 701213-36-7

HIV-1 attachment inhibitor

BMS-626529 is a potent HIV-1 attachment inhibitor. BMS-663068 is also the phosphonooxymethyl prodrug of BMS-626529 that targets HIV-1 gp120 and prevents its binding to CD4(+) T cells.

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Biological Activity

Cellular Effect

Cell Line Activity Value Description Reference
HCT-116 CC50 > 200 μM Cytotoxicity against human HCT116 cells after 6 days by XTT assay [PMID: 29271653]
HEK293 CC50 > 200 μM Cytotoxicity against HEK293 cells after 6 days by XTT assay [PMID: 29271653]
HeLa CC50 > 200 μM Cytotoxicity against human HeLa cells after 6 days by XTT assay [PMID: 29271653]
HeLa CC50 > 300 μM Cytotoxicity against human HeLa cells after 6 days by MTT assay [PMID: 26584882]
HEp-2 CC50 > 200 μM Cytotoxicity against human Hep2 cells after 6 days by XTT assay [PMID: 29271653]
HepG2 CC50 > 200 μM Cytotoxicity against human HepG2 cells after 6 days by XTT assay [PMID: 29271653]
HOS CC50 > 200 μM Cytotoxicity against HOS cells after 6 days by XTT assay [PMID: 29271653]
MCF7 CC50 > 200 μM Cytotoxicity against human MCF7 cells after 6 days by XTT assay [PMID: 29271653]
MT2 CC50 > 200 μM Cytotoxicity against human MT2 cells after 6 days by XTT assay [PMID: 29271653]
MT2 CC50 > 300 μM Cytotoxicity against human MT2 cells assessed as decrease in cell viability after 3 days by XTT assay [PMID: 29920093]
MT2 EC50 0.7 nM Antiviral activity against CXCR4-tropic HIV1 LAI infected in human MT2 cells by monogram phenosense entry assay [PMID: 26116177]
MT2 EC50 14.8 nM Antiviral activity against CXCR4-tropic HIV1 MN infected in human MT2 cells by monogram phenosense entry assay [PMID: 26116177]
MT2 EC50 16.2 nM Antiviral activity against CXCR4-tropic HIV1 3B infected in human MT2 cells by monogram phenosense entry assay [PMID: 26116177]
MT2 EC50 2.2 nM 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 Cytotoxicity against human NCI-H292 cells after 6 days by XTT assay [PMID: 29271653]
PBMC CC50 > 10 μM 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 Cytotoxicity against human PBMC after 6 days by XTT assay [PMID: 29271653]
SK-N-MC CC50 > 200 μM Cytotoxicity against human SK-N-MC cells after 6 days by XTT assay [PMID: 29271653]
TZM CC50 > 100 μM Cytotoxicity against human TZM-bl cells incubated for 3 days by MTS assay [PMID: 32031803]

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Specifications

Manufacturer Adooq Bioscience
Actions Inhibitor
CAS Number 701213-36-7
Applications HIV-1 attachment inhibitor
Formula C24H23N7O4
Molecular Weight 473.48
Synonyms BMS-626529
SMILES
CC1=NN(C=N1)C2=NC=C(C3=C2NC=C3C(=O)C(=O)N4CCN(CC4)C(=O)C5=CC=CC=C5)OC

Storage & Solubility

In Vitro Solubility

Reported Solubility

SolventReported Solubility
DMSO 92 mg/mL (194.3 mM)
Water Insoluble
Ethanol Insoluble

Preparing Stock Solutions

Stock preparation is unavailable for this product molecular weight.

Calculated stock concentrations do not establish solvent solubility. Refer to the reported solubility data for experimental guidance.

Storage

Store powder at -20°C, keep desiccated.
In powder form, the chemical is stable for 36 months.
In solution, store at -20°C and use within 1 month to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

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