SKU:K1323 | M. Wt:447.88 | ||
Formula:C23H23ClFNO5 | Solubility:No | ||
Purity:>99% | Storage:2 years at -20 degrees centigrade | ||
CAS No.:697761-98-1 | Synonyms:N/A | ||
Chemical NameN/A |
供货周期: | 一周 |
品牌: | |
规格: | 2mg |
货号: | K1323 |
CAS号: | 697761-98-1 |
SKU:K1323 | M. Wt:447.88 | ||
Formula:C23H23ClFNO5 | Solubility:No | ||
Purity:>99% | Storage:2 years at -20 degrees centigrade | ||
CAS No.:697761-98-1 | Synonyms:N/A | ||
Chemical NameN/A |
Description | Elvitegravir (GS-9137) | |||||
---|---|---|---|---|---|---|
Targets | HIV-1 IIIB | HIV-2 EHO | HIV-2 ROD | |||
IC50 | 0.7 nM | 2.8 nM | 1.4 nM | |||
In vitro | Elvitegravir (EVG, JTK-303/GS-9137) can inhibit HIV-1 IIIB, HIV-2 EHO and HIV-2 ROD with IC50 of 0.7 nM, 2.8 nM and 1.4 nM. Elvitegravir is predominantly metabolized via cytochrome P450 (CYP)3A4, along with minor pathways including glucuronidation via UGT1A1/3 and oxidative metabolism. Elvitegravir (EVG, JTK-303, GS-9137) currently being developed for the treatment of HIV-1 infection. Elvitegravir was more potent than raltegravir,a newly approved anti-AIDS drug. Elvitegravir can inhibit clinical HIV-2 isolates with IC50 of 0.7 nM while raltegravir inhibits those HIV-2 isolates with IC50 of 2.4 nM. Neither elvitegravir nor raltegravir could block disintegration. Elvitegravir (EVG) blocks the integration of HIV-1 cDNA through the inhibition of DNA strand transfer. Elvitegravir can inhibit 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. Clade-specific HIV-1 integrase polymorphisms do not reduce elvitegravir phenotypic susceptibility. | |||||
In vivo | Elvitegravir pharmacokinetic GMR was 6-7% higher following elvitegravir/r plus etravirine dosing versus elvitegravir/r. The coadministration of elvitegravir with the protease inhibitor ritonavir (a substantial CYP3A4 inhibitor) results in significantly enhanced bioavailability and a longer half-life than with elvitegravir alone, allowing for the once-daily dosing of elvitegravir. | |||||
Clinical Trials | N/A | |||||
Features | N/A |
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