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Elvitegravir(GS-9137,JTK-303)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Elvitegravir(GS-9137,JTK-303)图片
CAS NO:697761-98-1
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
Elvitegravir (also known as GS-9137, JTK-303, D06677 or EVG) is a potent HIV integrase inhibitor for HIV-1 IIIB, HIV-2 EHO and HIV-2 ROD with IC50 of 0.7 nM, 2.8 nM and 1.4 nM in cell-free assays, respectively. Elvitegravir is a monoketo acid modified from the distinct diketo acid moiety (DKA) motif and is used for the treatment of HIV infection. The drug received FDA approval on August 27, 2012 for use in adult patients starting HIV treatment for the first time as part of the fixed dose combination known as Stribild.
理化性质和储存条件
Molecular Weight (MW)447.88
FormulaC23H23ClFNO5
CAS No.697761-98-1
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 90 mg/mL (200.9 mM)
Water:<1 mg/mL
Ethanol: 35 mg/mL (78.1 mM)
Other info

Chemical Name: 6-[(3-Chloro-2-fluorophenyl)methyl]-1-[(2S)-1-hydroxy-3-methylbutan-2-yl]-7-methoxy-4-oxoquinoline-3-carboxylic acid

InChi Key: JUZYLCPPVHEVSV-LJQANCHMSA-N

InChi Code: InChI=1S/C23H23ClFNO5/c1-12(2)19(11-27)26-10-16(23(29)30)22(28)15-8-14(20(31-3)9-18(15)26)7-13-5-4-6-17(24)21(13)25/h4-6,8-10,12,19,27H,7,11H2,1-3H3,(H,29,30)/t19-/m1/s1

SMILES Code: O=C(C1=CN([C@@H](C(C)C)CO)C2=C(C=C(CC3=CC=CC(Cl)=C3F)C(OC)=C2)C1=O)O

SynonymsD06677; D-06677; D 06677; EVG, GS-9137; GS-9137; GS9137; GS 9137; JTK 303; JTK-303; JTK303; EVG; Stribild
实验参考方法
In Vitro

In vitro activity: Elvitegravir inhibits PBMC and PA with IC50 of 0.89 and 20 nM, respectively. Elvitegravir prevents the integration of HIV-1 cDNA through the inhibition of DNA strand transfer. Elvitegravir suppresses 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. Elvitegravir inhibits the replication of HIV-1 clinical isolates carrying NRTI, NNRTI, and PI resistance-associated genotypes. Elvitegravir inhibits the HIV replication at a step that occurs after reverse transcription but before proteolytic cleavage, consistent with the integration step. Elvitegravir inhibits the synthesis of strand transfer products with an IC50 of 54 nM. Elvitegravir blocks integration via the inhibition of IN-mediated strand transfer. Elvitegravir inhibits the integration of the HIV-based vector used as a positive control for the luciferase assay with an EC50 of 0.8 nM, as observed in the MAGI assay with HIV-1IIIB. Elvitegravir suppresses the replication of MLV infection with IC50 of 5.8 nM as well as that of the primate retrovirus SIV (IC50 = 0.5 nM), revealing that IN inhibitors have antiviral activity against a broad range of retroviruses. EVG 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.

In Vivo
Animal model
Formulation & Dosage
References

J Virol. 2008 Jan;82(2):764-74; Expert Rev Anti Infect Ther. 2012 Jan;10(1):13-20.