Elvitegravir (GS-9137)HIV-1 integrase inhibitor,potent CAS# 697761-98-1 |
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Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
| Cas No. | 697761-98-1 | SDF | Download SDF |
| PubChem ID | 23083982 | Appearance | Powder |
| Formula | C23H23ClFNO5 | M.Wt | 447.9 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Synonyms | GS-9137; JTK-303; EVG; D06677 | ||
| Solubility | DMSO : ≥ 50 mg/mL (111.64 mM) H2O : < 0.1 mg/mL (insoluble) *"≥" means soluble, but saturation unknown. | ||
| Chemical Name | 6-[(3-chloro-2-fluorophenyl)methyl]-1-(1-hydroxy-3-methylbutan-2-yl)-7-methoxy-4-oxoquinoline-3-carboxylic acid | ||
| SMILES | CC(C)C(CO)N1C=C(C(=O)C2=CC(=C(C=C21)OC)CC3=C(C(=CC=C3)Cl)F)C(=O)O | ||
| Standard InChIKey | JUZYLCPPVHEVSV-UHFFFAOYSA-N | ||
| Standard InChI | 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) | ||
| General tips | For 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. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| 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 | |||||
Elvitegravir (GS-9137) Dilution Calculator
Elvitegravir (GS-9137) Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.2326 mL | 11.1632 mL | 22.3264 mL | 44.6528 mL | 55.816 mL |
| 5 mM | 0.4465 mL | 2.2326 mL | 4.4653 mL | 8.9306 mL | 11.1632 mL |
| 10 mM | 0.2233 mL | 1.1163 mL | 2.2326 mL | 4.4653 mL | 5.5816 mL |
| 50 mM | 0.0447 mL | 0.2233 mL | 0.4465 mL | 0.8931 mL | 1.1163 mL |
| 100 mM | 0.0223 mL | 0.1116 mL | 0.2233 mL | 0.4465 mL | 0.5582 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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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.
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Broad antiretroviral activity and resistance profile of the novel human immunodeficiency virus integrase inhibitor elvitegravir (JTK-303/GS-9137).[Pubmed:17977962]
J Virol. 2008 Jan;82(2):764-74.
Integrase (IN), an essential enzyme of human immunodeficiency virus (HIV), is an attractive antiretroviral drug target. The antiviral activity and resistance profile in vitro of a novel IN inhibitor, elvitegravir (EVG) (also known as JTK-303/GS-9137), currently being developed for the treatment of HIV-1 infection are described. EVG 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. EVG-resistant variants were selected in two independent inductions, and a total of 8 amino acid substitutions in the catalytic core domain of IN were observed. Among the observed IN mutations, T66I and E92Q substitutions mainly contributed to EVG resistance. These two primary resistance mutations are located in the active site, and other secondary mutations identified are proximal to these primary mutations. The EVG-selected IN mutations, some of which represent novel IN inhibitor resistance mutations, conferred reduced susceptibility to other IN inhibitors, suggesting that a common mechanism is involved in resistance and potential cross-resistance. 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-870,810. EVG and L-870,810 both inhibited the replication of murine leukemia virus and simian immunodeficiency virus, suggesting that IN inhibitors bind to a conformationally conserved region of various retroviral IN enzymes and are an ideal drug for a range of retroviral infections.
