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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.
| Molecular Weight | 447.88 |
| Formula | C23H23ClFNO5 |
| CAS Number | 697761-98-1 |
| Solubility (25°C) | DMSO 90 mg/mL Ethanol 30 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Integrase Products |
|---|
| BMS-707035
BMS-707035 is an HIV-1 integrase (IN) inhibitor. HIV-1 integrase (IN) represents a therapeutically advantageous viral target to treat HIV/AIDS in the clinic. |
| Raltegravir
Raltegravir (MK-0518) is a potent integrase (IN) inhibitor for WT and S217Q PFV IN with IC50 of 90 nM and 40 nM, respectively. |
| MK-2048
MK-2048 is a potent inhibitor of integrase (IN) and INR263K with IC50 of 2.6 nM and 1.5 nM, respectively. |
| Dolutegravir
Dolutegravir (GSK1349572) is a two-metal-binding HIV integrase inhibitor with IC50 of 2.7 nM, modest activity against raltegravir-resistant signature mutants Y143R, Q148K, N155H, and G140S/Q148H. |
| Dolutegravir sodium
Dolutegravir sodium is a potent, second generation HIV integrase inhibitor (IC₅₀ = 2.7 nM) that displays potent antiviral activity. |
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