Elvitegravir (GS-9137)
(Synonyms: 埃替拉韦,Elvitegravir,GS9137) 目录号 : GC14996
An inhibitor of HIV-1 integrase
Cas No.:697761-98-1
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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. | |
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.
| Cas No. | 697761-98-1 | SDF | |
| 别名 | 埃替拉韦,Elvitegravir,GS9137 | ||
| 化学名 | 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 | ||
| 分子式 | C23H23ClFNO5 | 分子量 | 447.9 |
| 溶解度 | ≥ 20.35 mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
||
| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 2.2326 mL | 11.1632 mL | 22.3264 mL |
| 5 mM | 0.4465 mL | 2.2326 mL | 4.4653 mL |
| 10 mM | 0.2233 mL | 1.1163 mL | 2.2326 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。