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Elvitegravir

Cat. No. M1979
Elvitegravir Structure
Synonym:

GS-9137, EVG

Size Price Availability Quantity
10mg USD 100 In stock
50mg USD 390 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

Elvitegravir also inhibits PBMC and PA with IC50 of 0.89 and 20 nM, respectively. Elvitegravir (also known as JTK-303/GS-9137) blocked the integration of HIV-1 cDNA through the inhibition of DNA strand transfer. EVG inhibited 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. The replication capacity of EVG-resistant variants was significantly reduced relative to both wild-type virus and other IN inhibitor-resistant variants selected by L-870810. Elvitegravir (GS-9137) 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. According to the results of the phase II clinical trial, patients taking once-daily elvitegravir boosted by ritonavir had greater reductions in viral load after 24 weeks compared to individuals randomized to receive a ritonavir-boosted protease inhibitor. Elvitegravir is currengly in a Phase III clinical trial in the treatment of HIV-1 Infection.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
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.

Chemical Information
Molecular Weight 447.88
Formula C23H23ClFNO5
CAS Number 697761-98-1
Purity >99%
Solubility DMSO 90 mg/mL
Ethanol 30 mg/mL
Storage at -20°C
References

Co-formulated elvitegravir, cobicistat, emtricitabine, and tenofovir versus co-formulated efavirenz, emtricitabine, and tenofovir for initial treatment of HIV-1 infection: a randomised, double-blind, phase 3 trial, analysis of results after 48 weeks.
Sax PE, et al. Lancet. 2012 Jun 30;379(9835):2439-48. PMID: 22748591.

Broad antiretroviral activity and resistance profile of the novel human immunodeficiency virus integrase inhibitor elvitegravir (JTK-303/GS-9137).
Shimura K, et al. J Virol. 2008 Jan;82(2):764-74. PMID: 17977962.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Elvitegravir, GS-9137, EVG supplier, Integrase, inhibitors

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