1. Anti-infection
    Metabolic Enzyme/Protease
  2. HIV Integrase
    HIV

Elvitegravir (Synonyms: GS-9137; JTK-303; EVG; D06677)

Cat. No.: HY-14740 Purity: 99.78%
Handling Instructions

Elvitegravir is an HIV integrase inhibitor for HIV-1IIIB, HIV-2EHO and HIV-2ROD with IC50 of 0.7 nM, 2.8 nM and 1.4 nM, respectively.

Elvitegravir Chemical Structure

Elvitegravir Chemical Structure

CAS No. : 697761-98-1

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10 mM * 1 mL in DMSO $83 In-stock
10 mg $75 In-stock
50 mg $290 In-stock
100 mg $520 In-stock
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Description

Elvitegravir is an HIV integrase inhibitor for HIV-1IIIB, HIV-2EHO and HIV-2ROD with IC50 of 0.7 nM, 2.8 nM and 1.4 nM, respectively.

IC50 & Target

IC50: 0.7 nM (HIV-1IIIB), 2.8 nM (HIV-2EHO), 1.4 nM(HIV-2ROD)[1]

In Vitro

Elvitegravir (EVG) blocks the integration of HIV-1 cDNA through the inhibition of DNA strand transfer. Elvitegravir exerts potent anti-HIV activity against not only wild-type strains but also drug-resistant clinical isolates. Interestingly, Elvitegravir also shows antiviral activity against murine leukemia virus (MLV) and simian immunodeficiency virus (SIV). Elvitegravir shows potent antiviral activity against three laboratory strains of HIV, with EC50 values in the subnanomolar to nanomolar range. Next, the activity of Elvitegravir is evaluated against wild-type clinical isolates representing various subtypes of HIV-1. Elvitegravir suppresses the replication of all HIV-1 subtypes tested, with an antiviral EC50 ranging from 0.1 to 1.26 nM. Moreover, Elvitegravir suppresses the replication of HIV-1 clinical isolates carrying NRTI, NNRTI, and PI resistance-associated genotypes, as did a control IN inhibitor, the compound L-870,810. The cytotoxicities of these inhibitors are also determined using an MTT colorimetric assay. Mean values for the concentration that suppresses the viability of target cells by 50% for Elvitegravir and L-870,810 in PBMC obtained from three independent donors are 4.6±0.5 μM and 2.7±0.6 μM, respectively. Thus, Elvitegravir can suppress various HIV strains, including diverse HIV-1 subtypes and clinical isolates carrying multiple mutations associated with resistance to currently approved antiretroviral drugs[1].

Clinical Trial
Sponsor Condition Start Date Phase
Gilead Sciences Inc HIV-1 infection 2011-11-30 Phase 3
Gilead Sciences Inc HIV-1 infection 2013-09-30 Phase 3
Gilead Sciences Inc HIV-1 infection 2013-03-31 Phase 3
Gilead Sciences Inc HIV-1 infection 2013-03-31 Phase 3
Gilead Sciences Inc HIV-1 infection 2013-02-28 Phase 3
References
Preparing Stock Solutions
Concentration Volume (DMSO) Mass 1 mg 5 mg 10 mg
1 mM 2.2327 mL 11.1637 mL 22.3274 mL
5 mM 0.4465 mL 2.2327 mL 4.4655 mL
10 mM 0.2233 mL 1.1164 mL 2.2327 mL
Cell Assay
[1]

Elvitegravir (EVG) is prepared in DMSO and stored, and then diluted with appropriate medium before use[1].

MT-2 cells (2×105 cells) are infected with HIV-1 IIIB and then cultured in the presence of 0.5 nM or 0.1 nM Elvitegravir. Cultures are incubated at 37°C until an extensive cytopathic effect (CPE) is observed, and the culture supernatant is then harvested for further passage in fresh MT-2 cells. The concentration of Elvitegravir is increased when a significant CPE is observed. At the indicated passages, proviral DNA is extracted from infected MT-2 cells and then subjected to PCR, followed by direct population-based sequencing. Susceptibility to Elvitegravir at the indicated passages is determined using the MAGI assay or p24 production[1].

References
M.Wt

447.88

Formula

C₂₃H₂₃ClFNO₅

CAS No.

697761-98-1

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

Purity: 99.78%

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