Elvitegravir (GS-9137) (Synonyms: GS-9137, JTK-303) |
Catalog No.GC14996
One-Click Copy Product Info
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An inhibitor of HIV-1 integrase
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 697761-98-1
Sample solution is provided at 25 µL, 10mM.
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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
[1].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
[2].Peter K Quashie, Richard D Sloan and Mark A Wainberg. Novel therapeutic strategies targeting HIV integrase. BMC Medicine 2012; 10:34
[3].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.
Cell experiment: | MT-2 cells (2×105 cells) are infected with HIV-1 IIIB and then cultured in the presence of 0.5 nM or 0.1 nM Elvitegravir. Cultures are incubated at 37°C until an extensive cytopathic effect (CPE) is observed, and the culture supernatant is then harvested for further passage in fresh MT-2 cells. The concentration of Elvitegravir is increased when a significant CPE is observed. At the indicated passages, proviral DNA is extracted from infected MT-2 cells and then subjected to PCR, followed by direct population-based sequencing. Susceptibility to Elvitegravir at the indicated passages is determined using the MAGI assay or p24 production[1]. |
References: [1]. Shimura K, et al. Broad antiretroviral activity and resistance profile of the novel human immunodeficiency virus integrase inhibitor elvitegravir (JTK-303/GS-9137). J Virol. 2008 Jan;82(2):764-74. | |
| Cas No. | 697761-98-1 | SDF | |
| Synonyms | GS-9137, JTK-303 | ||
| Chemical Name | 6-[(3-chloro-2-fluorophenyl)methyl]-1-[(2S)-1-hydroxy-3-methylbutan-2-yl]-7-methoxy-4-oxoquinoline-3-carboxylic acid | ||
| Canonical 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 | ||
| Formula | C23H23ClFNO5 | M.Wt | 447.9 |
| Solubility | ≥ 20.35 mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.2326 mL | 11.1632 mL | 22.3264 mL |
| 5 mM | 446.5 μL | 2.2326 mL | 4.4653 mL |
| 10 mM | 223.3 μL | 1.1163 mL | 2.2326 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)