Elvitegravir

SKU: orb1305667

Description

Elvitegravir

Research Area

Infectious Disease & Virology, Protein Biochemistry

Key Properties

• CAS Number: 697761-98-1
• MW: 447.88
• Purity: 99.40%
• Formula: C₂₃H₂₃ClFNO₅
• SMILES: COC1=C(CC2=CC=CC(Cl)=C2F)C=C2C(=O)C(=CN(C(CO)C(C)C)C2=C1)C(O)=O
• Target: HIV Protease
• Solubility: H2O:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (7.37 mM);DMSO:82 mg/mL (183.08 mM);Ethanol:33 mg/mL (73.68 mM)

Bioactivity

• Target IC50:
  HIV-2 (ROD):1.4 nM|HIV-1 (IIIB):0.7 nM|HIV-2 (EHO):2.8 nM
• In Vivo:
  Elvitegravir inhibits the replication of MLV infection with an IC50 of 5.8 nM and also suppresses the primate retrovirus SIV with an IC50 of 0.5 nM, demonstrating its activity against multiple retroviruses due to IN inhibitor properties. It inhibits integrase activity with an IC50 of 6 nM and affects PBMC and PA with IC50 values of 0.89 nM and 20 nM, respectively. Additionally, Elvitegravir blocks the synthesis of chain transfer products with an IC50 of 54 nM by inhibiting integration via IN-regulated chain transfer. EVG exhibits antiviral activity without serum, with IC50 values ranging from 0.3 to 0.9 nM, targeting peripheral blood mononuclear cells and effectively inhibiting HIV-1 and HIV-2.
• Cell Research:
  Elvitegravir (EVG) is prepared in DMSO and stored, and then diluted with appropriate medium before use. 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.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

D 06677, D06677, D-06677, cDNA, Elvitegravir, EVG, GS9137, GS-9137, GS 9137, Inhibitor, Human immunodeficiency virus, HIV, HIV Integrase, HIV Protease, HIV-1 IIIB, HIV-1IIIB, HIV-2 EHO, HIV-2 ROD, HIV-2EHO, HIV-2ROD, HIVProtease, JTK 303, JTK303, JTK-303, inhibit

Compound Identifiers

PubChem CID

23083982