Elvitegravir (GS-9137)

Elvitegravir (GS-9137)

参考价:¥440
供货周期: 一周
品牌:
规格: 2mg
货号: K1323
CAS号: 697761-98-1
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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
Biological Activity
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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