化学性质
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 447.9 |
Cas No. | 697761-98-1 |
Formula | C23H23ClFNO5 |
Synonyms | Elvitegravir,GS9137 |
Solubility | insoluble in H2O; insoluble in EtOH; ≥20.35 mg/mL in DMSO |
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 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
资料参考
Elvitegravir(GS-9137,JTK-303),由不同的二酮酸部分(DKA)基序修饰而成的单酮酸,是一种有效的人类免疫缺陷病毒I型(HIV-1)整合酶抑制剂。HIV-1整合酶是一种酶,在HIV复制过程中,将病毒DNA整合进入宿主细胞的DNA上。Elvitegravir通过阻断病毒DNA的链转移和整合,抑制HIV-1整合酶的功能,从而阻止HIV的复制,使病毒DNA被细胞内的酶代谢掉。多项研究表明,elvitegravir不仅抑制多种HIV-1亚型的复制,还对鼠白血病病毒(MLV)和猿猴免疫缺陷病毒(SIV)展示了抗病毒活性。
参考文献:
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.
生物活性
描述 | Elvitegravir是一种有效的HIV-1整合酶抑制剂,IC50值为7.2 nM。 |
靶点 | HIV-I integrase | | | | | |
IC50 | 7.2 nM | | | | | |