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Fig. 1 · Structure
Cat. No.
A10347
CAS No.
697761-98-1
Formula
C23H23ClFNO5
Mol. Weight
447.9

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Elvitegravir (GS-9137)

Cat. No. A10347 CAS 697761-98-1

HIV integrase inhibitor

Elvitegravir (GS-9137) is a potent inhibitor of the strand-transfer step of integration mediated by human immunodeficiency virus type 1 (HIV-1) integrase.

In Stock

Publications for Elvitegravir

2 publications citing this product

  1. Lea El Khoury, .et al. , PeerJ Preprints, 2019, 7:e27833v1
  2. El Khoury L, .et al. , Biochem Biophys Res Commun, 2017, Jul 1;488(3):433-438 PMID: 28478035
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Biological Activity

Target & Activity

Target Activity Value
HIV-1 IIIB (Cell-free assay) 0.7 nM
HIV-2 ROD (Cell-free assay) 1.4 nM
HIV-2 EHO (Cell-free assay) 2.8 nM

Cellular Effect

Cell Line Activity Value Description Reference
C8166 EC50 0.00021 μM Antiviral activity against wild type HIV1 LAI-3B infected in human C8166 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay [PMID: 21862337]
C8166 EC50 0.00021 μM Antiviral activity against HIV1 LAI 3B infected in human C8166 cells assessed as protection against virus-induced cytopathic effect by MTT assay [PMID: 21763149]
C8166 EC50 0.001 μM Antiviral activity against HIV1 A17 harboring reverse transcriptase Y181C mutant infected in human C8166 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay [PMID: 21862337]
C8166 CC50 17.2 μM Cytotoxicity against human C8166 cells by MTT assay [PMID: 21862337]
C8166 CC50 17.2 μM Cytotoxicity against human C8166 cells by MTT assay [PMID: 21763149]
HEK-293T CC50 > 250 μM Cytotoxicity against human HEK293T cells assessed as cell growth inhibition by MTT assay [PMID: 36898139]
HeLa CC50 > 50 μM Cytotoxicity against human HeLa-CD4-LTR-beta-gal cells after 24 hrs by ATPlite reagent based luminescence analysis [PMID: 25961960]
HeLa CC50 > 50 μM Cytotoxicity against human HeLa cells expressing CD4-LTR-beta-gal after 24 hrs by ATPlite assay [PMID: 24684270]
HeLa EC50 0.0142 μM Antiviral activity against HIV1 3B infected in human HeLa cells expressing CD4-LTR-beta-gal assessed as inhibition of viral replication after 3 days by reporter gene assay [PMID: 24684270]
MT4 EC50 0.00037 μM Antiviral activity against HIV1 3B in MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay [PMID: 18665580]
MT4 EC50 0.0006 μM Antiviral activity against HIV 1 NL4.3 harboring integrase L74M mutant infected in human MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay [PMID: 18378713]
MT4 EC50 0.0007 μM Antiviral activity against HIV 1 RIN harboring integrase gene infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay [PMID: 18378713]
MT4 EC50 0.0008 μM Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay [PMID: 21227550]
MT4 EC50 0.0009 μM Antiviral activity against HIV 1 NL4.3 integrase S230N mutant infected in human MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay [PMID: 18378713]
MT4 EC50 0.001 μM Antiviral activity against HIV 1 3B infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay [PMID: 18378713]
MT4 EC50 0.0022 μM Antiviral activity against HIV1 harboring K103N/Y181C double mutant infected in human MT4 cells assessed as protection of cells from virus-induced cytopathic after 5 days by MTT assay [PMID: 25907370]
MT4 EC50 0.0031 μM Antiviral activity against wild-type HIV1 3B infected in human MT4 cells assessed as protection of cells from virus-induced cytopathic after 5 days by MTT assay [PMID: 25907370]
MT4 EC50 0.012 μM Antiviral activity against HIV 1 NL4.3 integrase E92Q mutant infected in human MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay [PMID: 18378713]
MT4 EC50 0.015 μM Antiviral activity against HIV 1 RIN harboring integrase gene infected in MT-4 cells assessed as inhibition of virus-induced cytopathic effect by MTT assay after 20 passages selected in presence of compound [PMID: 18378713]

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Specifications

Manufacturer Adooq Bioscience
Actions Inhibitor
CAS Number 697761-98-1
Applications HIV integrase inhibitor
Formula C23H23ClFNO5
Molecular Weight 447.9
Synonyms GS-9137
SMILES
CC(C)[C@@H](CO)N1C=C(C(=O)C2=CC(=C(C=C21)OC)CC3=C(C(=CC=C3)Cl)F)C(=O)O

Storage & Solubility

In Vitro Solubility

Reported Solubility

SolventReported Solubility
DMSO 85 mg/mL (189.78 mM)
Water Insoluble
Ethanol 33 mg/mL (73.67 mM)

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.

Publications

2 publications citing this product

  1. Lea El Khoury, .et al. , PeerJ Preprints, 2019, 7:e27833v1
  2. El Khoury L, .et al. , Biochem Biophys Res Commun, 2017, Jul 1;488(3):433-438 PMID: 28478035

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