Elvitegravir (GS-9137, JTK-303)

Elvitegravir (GS-9137, JTK-303) is an HIV integrase inhibitor for HIV-1 IIIB, HIV-2 EHO and HIV-2 ROD with IC50 of 0.7 nM, 2.8 nM and 1.4 nM in cell-free assays, respectively.

Price Stock Quantity  
In DMSO USD 160 In stock
USD 120 In stock
USD 470 In stock
Bulk Inquiry

Massive Discount Available

Free Overnight Delivery on all orders over $ 500.

Elvitegravir (GS-9137, JTK-303) Chemical Structure

Elvitegravir (GS-9137, JTK-303) Chemical Structure
Molecular Weight: 447.88

Validation & Quality Control

Customer Product Validation(6)

Quality Control & MSDS

Related Compound Libraries

Elvitegravir (GS-9137, JTK-303) is available in the following compound libraries:

Product Information

  • Compare Integrase Inhibitors
    Compare Integrase Products
  • Research Area
  • Elvitegravir (GS-9137, JTK-303) Mechanism

Product Description

Biological Activity

Description Elvitegravir (GS-9137, JTK-303) is an HIV integrase inhibitor for HIV-1 IIIB, HIV-2 EHO and HIV-2 ROD with IC50 of 0.7 nM, 2.8 nM and 1.4 nM in cell-free assays, respectively.
Targets HIV-1 IIIB [1]
(Cell-free assay)
HIV-2 ROD [1]
(Cell-free assay)
HIV-2 EHO [1]
(Cell-free assay)
IC50 0.7 nM 1.4 nM 2.8 nM
In vitro Elvitegravir inhibits PBMC and PA with IC50 of 0.89 and 20 nM, respectively. Elvitegravir prevents the integration of HIV-1 cDNA through the inhibition of DNA strand transfer. Elvitegravir suppresses the replication of HIV-1, including various subtypes and multiple-drug-resistant clinical isolates, and HIV-2 strains with a 50% effective concentration in the subnanomolar to nanomolar range. Elvitegravir inhibits the replication of HIV-1 clinical isolates carrying NRTI, NNRTI, and PI resistance-associated genotypes. Elvitegravir inhibits the 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. Elvitegravir blocks integration via the inhibition of IN-mediated strand transfer. [1] Elvitegravir inhibits the integration of the HIV-based vector used as a positive control for the luciferase assay with an EC50 of 0.8 nM, as observed in the MAGI assay with HIV-1IIIB. Elvitegravir suppresses the replication of MLV infection 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. EVG is active against HIV-1 and HIV-2 and has a serum-free antiviral IC50 of 0.3-0.9 nM in peripheral blood mononuclear cells. [2]
In vivo
Features

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Shimura K, et al. J Virol. 2008, 82(2), 764-774.

[2] Lampiris HW. Expert Rev Anti Infect Ther. 2012, 10(1), 13-20.

Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2015-06-27)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT02475135 Recruiting Healthy Janssen Sciences Ireland UC June 2015 Phase 1
NCT02470650 Not yet recruiting Patient Compliance|Antiretroviral Therapy Intolerance Juan A. Arnaiz|Hospital Clinic of Barcelona June 2015 Phase 4
NCT02351908 Not yet recruiting HIV St Stephens Aids Trust|Merck Sharp & Dohme Corp. February 2015 Phase 4
NCT02477527 Active, not recruiting HIV|AIDS|Sleep Disorders Midtown Medical Center, Tampa, FL|Gilead Sciences February 2015 Phase 4
NCT02198443 Not yet recruiting HIV Fundacion Clinic per a la Recerca Biomédica October 2014 Phase 4

view more

Chemical Information

Download Elvitegravir (GS-9137, JTK-303) SDF
Molecular Weight (MW) 447.88
Formula

C23H23ClFNO5

CAS No. 697761-98-1
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 90 mg/mL (200.94 mM)
Ethanol 35 mg/mL (78.14 mM)
Water <1 mg/mL (<1 mM)
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name (S)-6-(3-chloro-2-fluorobenzyl)-1-(1-hydroxy-3-methylbutan-2-yl)-7-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid

Customer Product Validation (6)


Click to enlarge
Rating
Source J Antimicrob Chemother 2011 66, 802-812. Elvitegravir (GS-9137, JTK-303) purchased from Selleck
Method PhA Flow Cytometry Efflux Assay
Cell Lines MDCKII-BCRP cells
Concentrations 0.001-1000 µM
Incubation Time
Results Elvitegravir and Vicriviroc increased PhA fluorescence in MDCKII-BCRP cells.

Click to enlarge
Rating
Source J Antimicrob Chemother 2011 66, 802-812. Elvitegravir (GS-9137, JTK-303) purchased from Selleck
Method Calcein assay
Cell Lines P388/dx cells
Concentrations 0.001-100 µM
Incubation Time
Results Vicriviroc and Elvitegravir clearly increased calcein fluorescence in P388dx and L-MDR1 cells, but not in the corresponding parental cell lines, which served as negative controls, indicating inhibition of ABCB1.

Click to enlarge
Rating
Source J Antimicrob Chemother 2011 66, 802-812. Elvitegravir (GS-9137, JTK-303) purchased from Selleck
Method Real-time RT–PCR
Cell Lines LS180 cells
Concentrations 10 µM
Incubation Time 3 d
Results For compounds(Elvitegravir, Rifampicin, Rifampicin and Maraviroc) with significant induction of ABCB1 mRNA expression at 10 mmol/L, induction was also quantified at the functional level after 3 days and 1 week of incubation. After 3 days of treatment, a trend towards increased ABCB1 activity was observed for Rifampicin and Elvitegravir. After 7 days ABCB1 activity was significantly increased by Elvitegravir, Vicriviroc and the positive control, Rifampicin.

Click to enlarge
Rating
Source Antim Ag Ch 2011 55, 42-49. Elvitegravir (GS-9137, JTK-303) purchased from Selleck
Method Virucidal activity assays
Cell Lines HeLa-T4 cell
Concentrations
Incubation Time 0-25 h
Results The addition of AZT could be delayed for about 4.8 h before 50% loss in potency was observed, whereas NVP required about 7.2 h to reveal this effect(Fig. 1A). These data reflect the need for AZT conversion to its active phosphorylated form, which NVP does not require. RAL addition could be postponed for about 10.2 h before 50% loss in activity was observed, whereas EVG required about 11.1 h. Titrating RAL and EVG over a 10-fold range (from 10× to 100× the EC95 ) did not significantly affect the resulting time windows (10.1 to 12.7 h for 50% inhibition) (Fig. B).

Click to enlarge
Rating
Source Antim Ag Ch 2011 55, 42-49. Elvitegravir (GS-9137, JTK-303) purchased from Selleck
Method virucidal activity assays
Cell Lines HeLa-T4 cell
Concentrations 1-100 µM
Incubation Time
Results EFV and EVG inhibited HIV-Luc infectivity, with EC50s of approximately 0.8 and 12 µM, respectively, whereas neither RAL nor NVP displayed significant activity.

Click to enlarge
Rating
Source 2010 Dr. Johanna Weiss of University Hospital Heidelberg. Elvitegravir (GS-9137, JTK-303) purchased from Selleck
Method Proliferation Assay
Cell Lines
Concentrations 0.01-1000 µM
Incubation Time
Results

Product Use Citation (10)

Tech Support & FAQs

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

* Indicates a Required Field

Related Integrase Products

  • Cabotegravir (GSK744, GSK1265744)

    Cabotegravir (GSK744, GSK1265744) is a long-acting HIV integrase inhibitor against a broad range of HIV subtypes, and inhibits the HIV-1 integrase catalyzed strand transfer reaction with IC50 of 3.0 nM. Phase 2.

  • Tenofovir Alafenamide (GS-7340)

    Tenofovir Alafenamide (GS-7340) is a prodrug of tenofovir, which is a reverse transcriptase inhibitor, used to treat HIV and Hepatitis B.

  • Raltegravir (MK-0518)

    Raltegravir (MK-0518) is a potent integrase (IN) inhibitor for WT and S217Q PFV IN with IC50 of 90 nM and 40 nM in cell-free assays, respectively.

    Features:The 1st approved human immunodeficiency virus type 1 (HIV-1) integrase inhibitor.

  • BMS-707035

    BMS-707035 is a specific HIV-I integrase (IN) inhibitor with IC50 of 15 nM. Phase 2.

  • Dolutegravir (GSK1349572)

    Dolutegravir (GSK1349572) is a two-metal-binding HIV integrase inhibitor with IC50 of 2.7 nM in a cell-free assay, modest activity against raltegravir-resistant signature mutants Y143R, Q148K, N155H, and G140S/Q148H.

    Features:A next-generation and two-metal-binding HIV integrase strand transfer inhibitor.

  • MK-2048

    MK-2048 is a potent inhibitor of integrase (IN) and INR263K with IC50 of 2.6 nM and 1.5 nM, respectively.

  • Maraviroc

    Maraviroc is a CCR5 antagonist for MIP-1α, MIP-1β and RANTES with IC50 of 3.3 nM, 7.2 nM and 5.2 nM in cell-free assays, respectively.

  • Tenofovir Disoproxil Fumarate

    Tenofovir Disoproxil Fumarate belongs to a class of antiretroviral drugs, it inhibits the activity of HIV reverse transcriptase by competing with the natural substrate deoxyadenosine 5’-triphosphate and, after incorporation into DNA, by DNA chain termination.

  • Zidovudine

    Zidovudine (ZDV) is a nucleoside analogue reverse transcriptase inhibitor, used to treat HIV.

Recently Viewed Items

Tags: buy Elvitegravir (GS-9137, JTK-303) | Elvitegravir (GS-9137, JTK-303) ic50 | Elvitegravir (GS-9137, JTK-303) price | Elvitegravir (GS-9137, JTK-303) cost | Elvitegravir (GS-9137, JTK-303) solubility dmso | Elvitegravir (GS-9137, JTK-303) purchase | Elvitegravir (GS-9137, JTK-303) manufacturer | Elvitegravir (GS-9137, JTK-303) research buy | Elvitegravir (GS-9137, JTK-303) order | Elvitegravir (GS-9137, JTK-303) mouse | Elvitegravir (GS-9137, JTK-303) chemical structure | Elvitegravir (GS-9137, JTK-303) mw | Elvitegravir (GS-9137, JTK-303) molecular weight | Elvitegravir (GS-9137, JTK-303) datasheet | Elvitegravir (GS-9137, JTK-303) supplier | Elvitegravir (GS-9137, JTK-303) in vitro | Elvitegravir (GS-9137, JTK-303) cell line | Elvitegravir (GS-9137, JTK-303) concentration | Elvitegravir (GS-9137, JTK-303) nmr
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description
Contact Us