Dolutegravir sodium|1051375-19-9|(度鲁特韦钠盐; S/GSK1349572 sodium)-陌孚医药/Medlife

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Dolutegravir sodium (Synonyms: 度鲁特韦钠盐; S/GSK1349572 sodium)

目录号: PL03296 纯度: ≥99%

CAS No. :1051375-19-9

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中文名称	Dolutegravir sodium
中文别名	度鲁特韦钠盐;2-氨基-5-溴-4-甲基烟酰胺;度鲁特韦纳;度鲁特韦钠;多特格伟钠盐;杜洛韦酯钠盐;杜鲁特韦钠盐;度鲁特维钠盐;度鲁特维钠盐(API);sodium;(4R,12aS)-9-[(2,4-difluorophenyl)methylcarbamoyl]-4-methyl-6,8-dioxo-3,4,12,12a-tetrahydro-2H-pyrido[5,6]pyrazino[2,6-b][1,3]oxazin-7-olate;多替拉韦钠盐
英文名称	Dolutegravir sodium
英文别名	dolutegravir sodium;Tivicay;GSK 1349572A;CHEMBL1213165;sodium (4R,12aS)-9-((2,4-difluorobenzyl)carbamoyl)-4-methyl-6,8-dioxo-3,4,6,8,12,12a-hexahydro-2H-pyrido[1',2',4,5]pyrazino[2,1-b][1,3]oxazin-7-olate;(4R,12aS)-N-(2,4-difluorobenzyl)-7-hydroxy-4-methyl-6,8-dioxo-3,4,6,8,12,12a-hexahydro-2H-pyrido[1',2':4,5]pyrazino-[2,1-b][1,3]oxazine-9-carboxamide sodium salt;CHEBI:76007;UNII-1Q1V9V5WYQ;Dolutegravir sodium [USAN];GSK1349572 sodiuM salt;GSK-1349572A;sodium;sodium,(4R,12aS)-9-[(2,4-difluorophenyl)methylcarbamoyl]-4-methyl-6,8-dioxo-3,4,12,12a-tetrahydro-2H-pyrido[5,6]pyrazino[2,6-b][1,3]oxazin-7-olate;(4R,12aS)-9-[(2,4-difluorophenyl)methylcarbamoyl]-4-methyl-6,8-dioxo-3,4,12,12a-tetrahydro-2H-pyrido[5,6]pyrazino[2,6-b][1,3]oxazin-7-olate;Dol;Duluvir sodium salt;(4R,12aS)-N-[(2,4-Difluorophenyl)methyl]-3,4,6,8,12,12a-hexahydro-7-hydroxy-4-methyl-6,8-dioxo-2H-pyrido[1',2':4,5]pyrazino[2,1-b][1,3]oxazine-9-carboxamide sodium salt (1:1);Dolutegravir sodium salt;Dolutegravi Sodium;Dolutegravir SodiuM ( API);Dolutegravir sodium(GSK1349572);(4R,12AS)-N-(2,4-difluorobenzyl)-7-hydroxy-4-methyl-6,8-dioxo-3,4,6,8,12,12a-hexahydro-2H-pyri;Sodium (4R,12aS)-9-((2,4-difluorobenzyl)carbamoyl)-4-methyl-6,8-dioxo-3,4,6,8,12,12a-hexahydro-2H-pyrido[1',2':4,5]pyrazino[2,1-b][1,3]oxazin-7-olate;Sodium;(4r,12as)-9-[(2,4-difluorophenyl)methylcarbamoyl]-4-methyl-6,8-dioxo-3,4,12,12a-tetrahydro-2h-pyrido[5,6]pyrazino[2,6-b][1,3]oxazin-7-olate;Dolutegravir Impurity 8;Dolutegravir (sodium);GSK1349572A;1Q1V9V5WYQ;Tivicay (TN);Dolut
Cas No.	1051375-19-9
分子式	C₂₀H₁₈F₂N₃NaO₅
分子量	441.36
包装储存	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

产品详情

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)。

生物活性

Dolutegravir sodium (S/GSK1349572 sodium) is a highly potent and orally bioavailable HIV integrase strand transfer inhibitor with an IC 50 of 2.7 nM for HIV-1 integrase-catalyzed strand transfer. Dolutegravir sodium (S/GSK1349572 sodium) inhibits HIV-1 viral replication with an IC 50 of 0.51 nM in peripheral blood mononuclear cells. Dolutegravir sodium (S/GSK1349572 sodium) retains a high potency against the HIV-1 Y143R, N155H, and G140S/Q148H mutants (EC 50 =3.6-5.8 nM).

性状

Solid

IC50 & Target[1][2]

IC50: 2.7 nM (HIV-1 integrase)

体外研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

ClinicalTrial

参考文献

[1]. Kobayashi M, et al. In Vitro antiretroviral properties of S/GSK1349572, a next-generation HIV integrase inhibitor. Antimicrob Agents Chemother. 2011 Feb;55(2):813-21.
[2]. Moss L, et al. The comparative disposition and metabolism of dolutegravir, a potent HIV-1 integrase inhibitor, in mice, rats, and monkeys. Xenobiotica. 2015 Jan;45(1):60-70.

溶解度数据	In Vitro: DMSO : ≥ 4.5 mg/mL (10.20 mM)H₂O : < 0.1 mg/mL (insoluble)

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。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。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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