产品名称

度鲁特韦(Dolutegravir)

一般描述

Dolutegravir is a Human Immunodeficiency Virus Integrase Strand Transfer Inhibitor.

别 称

(4R,12aS)-N-[(2,4-difluorophenyl)methyl]-7-hydroxy-4-methyl-6,8-dioxo-3,4,12,12a-tetrahydro-2H-pyrido[5,6]pyrazino[2,6-b][1,3]oxazine-9-carboxamide; GSK1349572

纯 度

≥98.0%(HPLC)

CAS NO.

1051375-16-6

分子式

C²⁰H¹⁹F²N³O⁵

分子量

419.38

适用范围

生物试剂，适用于细胞培养等

l  理化信息

外 观

固体

溶解性(25℃)

DMSO

≥50mg/mL(warmed)

乙醇

Insoluble

水

Insoluble

l  生物学信息

生物活性/药理作用

Dolutegravir is an orally bioavailable integrase strand-transfer inhibitor (INSTI), with activity against human immunodeficiency virus type 1(HIV-1) infection. Upon oral administration, dolutegravir binds to the active site of integrase, an HIV enzyme that catalyzes the transfer of viral genetic material into human chromosomes. This prevents integrase from binding to retroviral deoxyribonucleic acid (DNA), and blocks the strand transfer step, which is essential for the HIV replication cycle. This prevents HIV-1. Dolutegravir is a two-metal-binding HIV integrase inhibitor with IC50 of 2.7 nM in a cell-free assay, modest activity against raltegravir-resistant signature mutants Y143R, Q148K, N155H, and G140S/Q148H.

l  存储

存储温度

-20℃

l  注意事项及免责声明

本产品仅用于实验研究，不得作为药物使用，不得用于家用或其它用途。

l  参考文献

1.    http://www.drugbank.ca

2.    https://ncit.nci.nih.gov

3.    https://www.ncbi.nlm.nih.gov