Molecular Formula | C23H23ClFNO5
|
Molar Mass | 447.88 |
Density | 1.357±0.06 g/cm3(Predicted) |
Melting Point | 93-96°C |
Boling Point | 623.6±55.0 °C(Predicted) |
Solubility | DMSO ≥86mg/mL Water <1.2mg/mL Ethanol ≥85mg/mL |
Appearance | Form Solid, color Off-White to Pale Yellow |
Color | Off-White to Pale Yellow |
pKa | 0.44±0.20(Predicted) |
Storage Condition | Refrigerator |
Physical and Chemical Properties | Bioactive Elvitegravir (GS-9137, JTK-303) is an HIV inhibitor that acts on HIV-1 IIIB,HIV-2 EHO and HIV-2 ROD. IC50 is 0.7,2.8 and 1.4 nM respectively in cell-free tests. |
Use | Use Etigavir is a class of integrase inhibitors and is the first quinolone anti-AIDS drug. |
In vitro study | Elvitegravir inhibits integrase activity with an IC50 of 6 nM. Elvitegravir inhibited PBMC and PA with IC50 of 0.89 and 20 nM, respectively. Elvitetravir inhibited HIV-1 of cDNA integration by inhibiting DNA strand transfer. Subna molar to nanomolar levels elvitetravir inhibited HIV-1 replication, including multiple subtypes and multiple drug-resistant clinical isolates, and HIV-2 strains, at an effective concentration of 50%. Elvitetravir inhibits HIV-1 clinical isolates carrying anti-NRTI, NNRTI, and PI-related genotypes. Following reverse transcription, before protein cleavage, elvitetravir inhibits HIV replication, consistent with the integration step. Elvitetravir inhibited the synthesis of chain transfer products with an IC50 of 54 nM. Elvitetravir inhibits integration by inhibiting IN-regulated chain transfer. Elvitegravir inhibited the integration of HIV vector and served as a positive control for luciferase experiments with an EC50 of 0.8 nM. Elviteetravir inhibits the replication of MLV infection with an IC50 of 5.8 nM and also inhibits reverse transcription of Virus SIV(IC50 of 0.5 nM) IN primates, indicating that IN inhibitors have activity against multiple reverse transcription Virus. EVG acts on peripheral blood mononuclear cells, effectively acts on HIV-1 and HIV-2, and has serum-free antiviral activity with IC50 of 0.3-0.9 nM. |