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Elvitegravir (GS-9137)

In stock
Catalog No.
A4070
HIV-1 integrase inhibitor,potent
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$83.00
In stock
10mg
$75.00
In stock
50mg
$290.00
In stock
100mg
$520.00
In stock

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Background

Elvitegravir (also known as GS-9137 or JTK-303), a monoketo acid modified from the distinct diketo acid moiety (DKA) motif, is a potent inhibitor of human immunodeficiency virus type I (HIV-1) integrase, an enzyme integrating the viral DNA into the cellular DNA of the host during HIV replication. Elvitegravir inhibits the function of HIV-1 integrase through blocking viral DNA strand transfer and integration, which prevents the replication of HIV and subsequently allows viral DNA to be metabolized by cellular enzymes. Multiple studies indicate that elvitegravir not only inhibits the replication of a variety of subtypes of HIV-1 but also exhibits antiviral activity against murine leukemia virus (MLV) and simian immunodeficirncy virus (SIV).

Reference

Janice Soo Fern Lee, Alexandra Calmy, Isabelle Andrieux-Meyer, and Nathan Ford. Review of the safty, efficacy, and pharmacokinetics of elviteravir with an emphasis on resource-limited settings. HIV/AIDS- Research and Palliative Care 2012; 4: 5-15

Peter K Quashie, Richard D Sloan and Mark A Wainberg. Novel therapeutic strategies targeting HIV integrase. BMC Medicine 2012; 10:34

Kazuya Shimura, Eiichi Kodama, Yasuko Sakagami, Yuji Matsuzaki, Wataru Watanabe, Kazunobu Yamataka, Yasuo Watanabe, Yoshitsugu Ohata, Satoki Doi, Motohide Sato, Mitsuki Kano, Satoru Ikeda, and Masao Matsuoka. Broad antiretroviral activity and resistance profile of the novel human innunodeficiency virus integrase inhibitor elvitegravir. (JTK-303/GS-9137). Journal of Virology 2008; 764-774.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt447.9
Cas No.697761-98-1
FormulaC23H23ClFNO5
SynonymsElvitegravir,GS9137
Solubility≥20.35 mg/mL in DMSO, <2.65 mg/mL in EtOH, <2.45 mg/mL in H2O
Chemical Name6-[(3-chloro-2-fluorophenyl)methyl]-1-[(2S)-1-hydroxy-3-methylbutan-2-yl]-7-methoxy-4-oxoquinoline-3-carboxylic acid
SDFDownload SDF
Canonical SMILESCC(C)C(CO)N1C=C(C(=O)C2=CC(=C(C=C21)OC)CC3=C(C(=CC=C3)Cl)F)C(=O)O
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Biological Activity

Description Elvitegravir is a potent inhibitor of HIV-I integrase with IC50 value of 7.2 nM.
Targets HIV-I integrase          
IC50 7.2 nM          

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