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Elvitegravir (GS-9137) Chemical Structure
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Biological Activity
| Information | Elvitegravir (EVG, JTK-303, GS-9137) is an inhibitor of the integrase enzyme and inhibits HIV-1 IIIB, HIV-2 EHO and HIV-2 ROD with IC50 values of 0.7 nM, 2.8 nM and 1.4 nM, respectively. | |||||
|---|---|---|---|---|---|---|
| Targets | HIV-1IIIB | HIV-2EHO | HIV-2ROD | |||
| IC50 | 0.7 nM | 2.8 nM | 1.4 nM [1] | |||
| In vitro | Elvitegravir inhibits the replication of HIV-1, including its various subtypes and multiple-drug-resistant clinical isolates and HIV-2 strains with a 50% effective concentration in the subnanomolar to nanomolar range. Elvitegravir also suppresses the replication of HIV-1 clinical isolates carrying NRTI, NNRTI, and PI resistance-associated genotypes. Elvitegravir inhibits the viability of PBMC by 50% at 4.6 µM. [1] Elvitegravir inhibits the integration of HIV-1 cDNA into the host genome by blocking IN-mediated DNA strand transfer. Elvitegravir inhibits HIV replication at a step that occurs after reverse transcription but before proteolytic cleavage, consistent with the integration step. Elvitegravir inhibits the synthesis of strand transfer products with an IC50 of 54 nM. The integration of the HIV-based vector used as a positive control for the luciferase assay is inhibited by Elvitegravir with EC50 of 0.8 nM, as observed in the MAGI assay with HIV-1IIIB. Elvitegravir suppresses the replication of MLV DNA with IC50 of 5.8 nM as well as that of the primate retrovirus SIV (IC50 = 0.5 nM), revealing that IN inhibitors have antiviral activity against a broad range of retroviruses. [2] | |||||
| In vivo | ||||||
| Clinical Trials | Elvitegravir is currently under Phase III clinical trial for the treatment of HIV-1 infection. | |||||
| Features | ||||||
Protocol
Kinase Assay: [1]
| Galactosidase indicator (MAGI) assay | Inhibitory effects of Elvitegravir on HIV infection is determined using multinuclear activation of a galactosidase indicator (MAGI) assay. Briefly, the target cells (HeLa-CD4-LTR-β-gal; 104 cells/well) are plated in 96-well flat microtiter culture plates. On the following day, the cells are inoculated with the HIV-1 clones (60 MAGI U/well, giving 60 blue cells after 48 hours of incubation) and cultured in the presence of various concentrations of Elvitegravir in fresh medium. Forty-eight hours after viral exposure, all the blue cells stained with X-Gal (5-bromo-4-chloro-3-indolyl-β-d-galactopyranoside) are counted in each well. The activity of Elvitegravir is determined as the concentration that blocked HIV-1 replication by 50% (50% effective concentration [EC50]). |
|---|
Chemical Information
| Molecular Weight (WM): | 447.88 |
|---|---|
| Formula: | C23H23ClFNO5 |
| CAS No.: | 697761-98-1 |
| Synonyms: |
N/A
|
| Dissolve in (25°C): | DMSO ≥90mg/mL |
| Water <1mg/mL | |
| Ethanol ≥90mg/mL | |
| Storage: | 2 years-20°CPowder |
| 1 week-4°Cin DMSO | |
| 1 month-80°in DMSO |
Quality Control & MSDS
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Selleck's high quality products have been used in several published research findings, including the following:
Potential of novel antiretrovirals to modulate expression and function of drug transporters in vitro.
Identification and Characterization of Persistent Intracellular Human Immunodeficiency Virus Type 1 Integrase Strand Transfer Inhibitor Activity.
Differential Sensitivities of Retroviruses to Integrase Strand Transfer Inhibitors.
Susceptibility of the human retrovirus XMRV to antiretroviral inhibitors.
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Cells were treated with the indicated concentrations of Elvitegravir. - Cells were treated with the indicated concentrations of Elvitegravir.
Data independently produced by Dr Johanna Weiss of University Hospital Heidelberg Elvitegravir (GS-9137) purchased from Selleck
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PhA efflux in MDCKII-BCRP cells. Concentration-dependent inhibition of BCRP/ABCG2 by elvitegravir and vicriviroc. Each curve depicts one representative experiment of a series of three or four; each concentration was tested in 30000 cells.
PhA efflux in MDCKII-BCRP cells. Concentration-dependent inhibition of BCRP/ABCG2 by elvitegravir and vicriviroc. Each curve depicts one representative experiment of a series of three or four; each concentration was tested in 30000 cells.
Data from [J Antimicrob Chemother 2011.January;66:802-812] Elvitegravir (GS-9137) purchased from Selleck
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mdr1a/b and ABCB1 inhibition measured by calcein assay. Concentration-dependent effects of elvitegravir and vicriviroc on calcein accumulation in P388/dx cells (a) and L-MDR1 cells (b). Each curve depicts one representative experiment of a series of three or four. Data are expressed as means+SEM.
mdr1a/b and ABCB1 inhibition measured by calcein assay. Concentration-dependent effects of elvitegravir and vicriviroc on calcein accumulation in P388/dx cells (a) and L-MDR1 cells (b). Each curve depicts one representative experiment of a series of three or four. Data are expressed as means+SEM.
Data from [J Antimicrob Chemother 2011.January;66:802-812] Elvitegravir (GS-9137) purchased from Selleck
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Effect of antiretrovirals and positive control rifampicin (at 10 mmol/L) on ABCB1 function in LS180 cells after 3 and 7 days (d) of treatment. ABCB1 function was normalized to the medium control. Data are expressed as means+SEM for n¼4. **P,0.01.
Effect of antiretrovirals and positive control rifampicin (at 10 mmol/L) on ABCB1 function in LS180 cells after 3 and 7 days (d) of treatment. ABCB1 function was normalized to the medium control. Data are expressed as means+SEM for n¼4. **P,0.01.
Data from [J Antimicrob Chemother 2011.January;66:802-812] Elvitegravir (GS-9137) purchased from Selleck
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Functional windows of antiviral drug action. (A) At the indicated times, 10-fold EC95 adjusted levels of RAL, EVG, AZT, or NVP were added to HIV-Luc-infected cultures. Cells were lysed at 48 h postinfection, and luciferase activities are expressed as the percentage of the response in non-drug-treated cells. (B) Results of an experiment similar to that in panel A, except cells were treated with 10 the EC95 of RAL, 100 the EC95 of RAL, 10 the EC95 of EVG, or 100 the EC95 of EVG at the indicated times. Numbers indicate the time (in h) required for 50% inhibition compared to the no-drug control (dashed lines).
Functional windows of antiviral drug action. (A) At the indicated times, 10-fold EC95 adjusted levels of RAL, EVG, AZT, or NVP were added to HIV-Luc-infected cultures. Cells were lysed at 48 h postinfection, and luciferase activities are expressed as the percentage of the response in non-drug-treated cells. (B) Results of an experiment similar to that in panel A, except cells were treated with 10 the EC95 of RAL, 100 the EC95 of RAL, 10 the EC95 of EVG, or 100 the EC95 of EVG at the indicated times. Numbers indicate the time (in h) required for 50% inhibition compared to the no-drug control (dashed lines).
Data from [Antimicrobial Agents and Chemotherapy 2011.January;55:42-49] Elvitegravir (GS-9137) purchased from Selleck
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HIV-Luc was preincubated with the indicated level of drug for 1 h prior to 2 min of MNP-mediated infection. Extensively washed cultures were incubated in the absence of drug for 2 days prior to cell lysis and luciferase assays. The NN-luc control virus was omitted from the virucidal activity assays.
HIV-Luc was preincubated with the indicated level of drug for 1 h prior to 2 min of MNP-mediated infection. Extensively washed cultures were incubated in the absence of drug for 2 days prior to cell lysis and luciferase assays. The NN-luc control virus was omitted from the virucidal activity assays.
Data from [Antimicrobial Agents and Chemotherapy 2011.January;55:42-49] Elvitegravir (GS-9137) purchased from Selleck
- We are happy with the Elvitegravir, it is working as expected in our experiments!
Geoffrey GottliebDivision of Allergy & Infectious Diseases Department of Medicine University of Washington
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| Cells were treated with the indicated concentrations of Elvitegravir. |
Data independently produced by Dr Johanna Weiss of University Hospital Heidelberg
PhA efflux in MDCKII-BCRP cells. Concentration-dependent inhibition of BCRP/ABCG2 by elvitegravir and vicriviroc. Each curve depicts one representative experiment of a series of three or four; each concentration was tested in 30000 cells.
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Data from [J Antimicrob Chemother 2011.January;66:802-812]
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