MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。

Dolutegravir sodium

CAS No. : 1051375-19-9

MCE 站：Dolutegravir sodium

产品活性：Dolutegravir sodium (S/GSK1349572 sodium) 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，Dolutegravir sodium (S/GSK1349572 sodium) 抑制 HIV-1 病毒在外周血单个核细胞中的复制，IC₅₀ 为 0.51 nM。Dolutegravir sodium (S/GSK1349572 sodium) 对 Y143R，N155H 和 G140S/Q148H 突变体也保持高效 (EC₅₀=3.6-5.8 nM)。

研究领域：Metabolic Enzyme/Protease  |  Anti-infection

作用靶点：HIV Integrase  |  HIV

In Vitro: The EC₅₀ of Dolutegravir (S/GSK1349572) against HIV-1 is 0.51 nM in PBMCs, 0.71 nM in MT-4 cells, and 2.2 nM in the PHIV assay, which uses a pseudotyped self-inactivating virus. The 50% cytotoxic concentrations (CC₅₀) for Dolutegravir in proliferating IM-9, U-937, MT-4, and Molt-4 cells are 4.8, 7.0, 14, and 15 μM, respectively. In unstimulated and stimulated PBMCs, the CC₅₀ are 189 μM and 52 μM, respectively. Based on the EC₅₀ of Dolutegravir against HIV-1 in PBMCs (i.e., 0.51 nM), this translates to a cell-based therapeutic index of at least 9,400.

In Vivo: Following a single intravenous (IV) administration of Dolutegravir, the plasma clearance is low in rats (0.23?mL/min/kg) and monkeys (2.12?mL/min/kg). The half-lives in the rat and monkey are similar, approximately 6?h, and the steady-state volume of distribution (V_SS) is low. Following oral administration, Dolutegravir is rapidly absorbed with a high oral bioavailability when administered as a solution to fasted male rats and a single monkey (75.6 and 87.0%, respectively). Dolutegravir exposure (C_max and AUC) increased with increasing dose following oral administration of a suspension to non-fasted rats up to 250?mg/kg and non-fasted monkeys up to 50?mg/kg, although the increase is less than proportional.

相关产品：Drug Repurposing Compound Library Plus  |  FDA-Approved Drug Library Plus  |  FDA-Approved Drug Library Mini  |  Bioactive Compound Library Plus  |  Anti-Infection Compound Library  |  Metabolism/Protease Compound Library  |  FDA-Approved Drug Library  |  Antiviral Compound Library  |  Drug Repurposing Compound Library  |  NMPA-Approved Drug Library  |  Orally Active Compound Library  |  FDA Approved & Pharmacopeial Drug Library  |  Doxorubicin hydrochloride  |  Chloroquine  |  5-Fluorouracil  |  Valproic acid  |  (-)-Epigallocatechin Gallate  |  Shikonin  |  Ivermectin  |  Ebselen  |  Kaempferol  |  Flavopiridol  |  Maraviroc  |  Hydroxyurea  |  Dimethyl fumarate  |  Baicalin  |  Probenecid  |  Ritonavir  |  Fasudil Hydrochloride  |  Lopinavir  |  Betulinic acid  |  Lamivudine  |  Rolipram  |  Nelfinavir Mesylate  |  Oltipraz  |  Saquinavir  |  Rottlerin  |  Cepharanthine  |  Zidovudine

品牌介绍:
•   MCE (MedChemExpress) 拥有数百种全球独家化合物，我们致力于为全球科研客户提供*新*全的高品质小分子活性化合物；
•   10,000 多种高选择性抑制剂、激动剂涉及各热门信号通路及疾病领域；
•   设有专业的实验中心和严格的质控、验证体系；
•   提供 LC/MS、NMR、HPLC、手性分析、元素分析等各项质检报告，确保产品的高纯度、高品质；
•   产品的生物活性多经各国客户实验验证；
•   Nature, Cell, Science 等多种期刊及制药收录了MCE客户的科研成果；
•   专业团队跟踪*新的制药及生命科学研究进展，为您提供全球*新的活性化合物；
•   与世界各大制药公司及知名科研机构建立了长期的合作。