Elvitegravir (GS-9137)

目录号: GC14996纯度: >99.50%同义词: 埃替拉韦,Elvitegravir,GS9137
An inhibitor of HIV-1 integrase

Elvitegravir (GS-9137)
Cas No.: 697761-98-1
规格价格库存数量操作
10mg¥515.00现货
1
50mg¥2,258.00现货
1
100mg¥3,780.00现货
1
10mM (in 1mL DMSO)¥641.00现货
1

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产品描述 Description

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.

实验参考方法 Experimental Reference Method

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.

产品文档 Product Documents

Purity:>99.50%

化学性质Chemical Properties

CAS 号
697761-98-1
同义词
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
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 g/mol
溶解性
≥ 20.35 mg/mL in DMSO
保存条件
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°C,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。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

g/mol