dolutegravir

Dolutegravir (GSK1349572) 是口服HIV 整合酶链转移高效抑制剂，抑制 HIV-1 病毒在外周血单个核细胞中的复制。它对耐拉替拉韦的特征突变体 Y143R、Q148K、N155H 和 G140S Q148H 具有中等活性。

Dolutegravir sodium (GSK-1349572A) 是一种高效、口服的 HIV 整合酶链转移抑制剂，在 HIV-1 整合酶催化的链转移中的 IC50值为 2.7 nM， 抑制 HIV-1 病毒在外周血单个核细胞中的复制，IC50为 0.51 nM。它对 Y143R，N155H 和 G140S Q148H 突变体也保持高效。

Dolutegravir intermediate-1 (1-(2,2-dimethoxyethyl)-5-methoxy-6-(methoxycarbonyl)-4-oxo-1,4-dihydropyridine-3-carboxylic acid) 是 Dolutegravir 的一种新合成中间体。 它是一种整合酶抑制剂，有潜力研究人类免疫缺陷病毒 (HIV)-1 感染。

Dolutegravir M1 is a metabolite of the HIV integrase inhibitor dolutegravir .1It is formed primarily by the cytochrome P450 (CYP) isoforms CYP1A1 and CYP1B1. 1.Zhu, J., Wang, P., Li, F., et al.CYP1A1 and 1B1-mediated metabolic pathways of dolutegravir, an HIV integrase inhibitorBiochem. Pharmacol.158174-184(2018)

Dolutegravir O-β-D-glucuronide is a metabolite of the HIV integrase inhibitor dolutegravir .1It is formed from dolutegravir primarily by the UDP-glucuronosyltransferase (UGT) isoform UGT1A1in vivobut is also metabolized by UGT1A9 in human liver and kidney microsomes and UGT1A3 in human intestinal microsomes.2,1 1.Liu, S.N., Lu, J.B., Watson, C.J.W., et al.Mechanistic assessment of extrahepatic contributions to glucuronidation of integrase strand transfer inhibitorsDrug Metab. Dispos.47(5)535-544(2019) 2.Reese, M.J., Savina, P.M., Generaux, G.T., et al.In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitorDrug Metab. Dispos.41(2)353-361(2013)

Dolutegravir RR Isomer is an isomer of Dolutegravir -- a second generation HIV-1 integrase strand transfer inhibitor. Dolutegravir has been shown to potently inhibit HIV replication in cells such as peripheral blood mononuclear cells (PBMCs), MT-4 cells and CIP4 cells infected with a self-inactivating PHIV lentiviral vector.

Dolutegravir SR Isomer is an isomeric derivative of Dolutegravir -- a second generation HIV-1 integrase strand transfer inhibitor. Dolutegravir has been shown to potently inhibit HIV replication in cells such as peripheral blood mononuclear cells (PBMCs), MT-4 cells and CIP4 cells infected with a self-inactivating PHIV lentiviral vector.

Baloxavir (S-033447) 是衍生自前药 Baloxavir marboxil，是流感病毒聚合酶 PA 亚基的一流帽依赖性核酸内切酶抑制剂。它抑制病毒 RNA 的转录和复制，具有强大的抗病毒活性。