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

目录号: HY-13238A 纯度: 99.97%: FAQs
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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)。

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Dolutegravir sodium Chemical Structure

CAS No. : 1051375-19-9

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MCE 顾客使用本产品发表的 24 篇科研文献

Proliferation Assay

: Dolutegravir sodium purchased from MCE. Usage Cited in: Antivir Ther. 2017;22(8):645-657. [Abstract]; Dolutegravir (DTG) and MVC+DTG significantly increase the SIRT1 level by respectively, 9% and 18%.

: Dolutegravir sodium purchased from MCE. Usage Cited in: Cell Physiol Biochem. 2016 Jul 21;39(2):639-650. [Abstract]; Arithmetic means±SEM (n=19) of erythrocyte annexin-V-binding following incubation for 48 hours to Ringer solution without (white bar) or with (black bars) Dolutegravir (4.77-19.08 µM). For comparison, the effect of the solvent DMSO is shown (grey bar).

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HIV HIV-1 HIV-2

生物活性
实验参考方法
纯度 & 产品资料
参考文献

生物活性

Dolutegravir sodium (S/GSK1349572 sodium) is a highly potent and orally bioavailable HIV integrase strand transfer inhibitor with an IC₅₀ of 2.7 nM for HIV-1 integrase-catalyzed strand transfer. Dolutegravir sodium (S/GSK1349572 sodium) inhibits HIV-1 viral replication with an IC₅₀ 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 (EC₅₀=3.6-5.8 nM)^[1]^[2].

IC₅₀ & Target

HIV-1

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
IM-9	CC₅₀	4.8 μM Compound: S/GSK-1349572	Cytotoxicity against human IM9 cells after 2 days by Cell titer Glo luminescent assay Cytotoxicity against human IM9 cells after 2 days by Cell titer Glo luminescent assay	[PMID: 21115794]
MOLT-4	CC₅₀	15 μM Compound: S/GSK-1349572	Cytotoxicity against human MOLT4 cells after 2 days by Cell titer Glo luminescent assay Cytotoxicity against human MOLT4 cells after 2 days by Cell titer Glo luminescent assay	[PMID: 21115794]
MT2	EC₅₀	0.26 nM Compound: S/GSK-1349572	Antiviral activity against Human immunodeficiency virus 1 3B infected in human MT2 cells assessed as inhibition of virus induced cytopathic effect measured after 2 to 3 days by PCR Antiviral activity against Human immunodeficiency virus 1 3B infected in human MT2 cells assessed as inhibition of virus induced cytopathic effect measured after 2 to 3 days by PCR	[PMID: 21115794]
MT2	EC₅₀	0.26 nM Compound: S/GSK-1349572	Antiviral activity against Human immunodeficiency virus 1 3B harboring integrase T124A mutant gene infected in human MT2 cells assessed as inhibition of virus induced cytopathic effect selected after 14 passages measured after 2 to 3 days by PCR Antiviral activity against Human immunodeficiency virus 1 3B harboring integrase T124A mutant gene infected in human MT2 cells assessed as inhibition of virus induced cytopathic effect selected after 14 passages measured after 2 to 3 days by PCR	[PMID: 21115794]
MT2	EC₅₀	0.26 nM Compound: S/GSK-1349572	Antiviral activity against Human immunodeficiency virus 1 3B harboring integrase T124A/S153F mutant gene infected in human MT2 cells assessed as inhibition of virus induced cytopathic effect selected after 28 passages measured after 2 to 3 days by PCR Antiviral activity against Human immunodeficiency virus 1 3B harboring integrase T124A/S153F mutant gene infected in human MT2 cells assessed as inhibition of virus induced cytopathic effect selected after 28 passages measured after 2 to 3 days by PCR	[PMID: 21115794]
MT2	EC₅₀	0.26 nM Compound: S/GSK-1349572	Antiviral activity against Human immunodeficiency virus 1 3B harboring integrase T124A/S153F mutant gene infected in human MT2 cells assessed as inhibition of virus induced cytopathic effect selected after 42 passages measured after 2 to 3 days by PCR Antiviral activity against Human immunodeficiency virus 1 3B harboring integrase T124A/S153F mutant gene infected in human MT2 cells assessed as inhibition of virus induced cytopathic effect selected after 42 passages measured after 2 to 3 days by PCR	[PMID: 21115794]
MT2	EC₅₀	1.3 nM Compound: S/GSK-1349572	Antiviral activity against Human immunodeficiency virus 1 3B harboring integrase T124A/S153F mutant gene infected in human MT2 cells assessed as inhibition of virus induced cytopathic effect selected after 56 passages measured after 2 to 3 days by PCR Antiviral activity against Human immunodeficiency virus 1 3B harboring integrase T124A/S153F mutant gene infected in human MT2 cells assessed as inhibition of virus induced cytopathic effect selected after 56 passages measured after 2 to 3 days by PCR	[PMID: 21115794]
MT2	EC₅₀	1.3 nM Compound: S/GSK-1349572	Antiviral activity against Human immunodeficiency virus 1 3B harboring integrase S153Y/L101I/T124A/S153F mutant gene infected in human MT2 cells assessed as inhibition of virus induced cytopathic effect selected after 70 passages measured after 2 to 3 day Antiviral activity against Human immunodeficiency virus 1 3B harboring integrase S153Y/L101I/T124A/S153F mutant gene infected in human MT2 cells assessed as inhibition of virus induced cytopathic effect selected after 70 passages measured after 2 to 3 day	[PMID: 21115794]
MT2	EC₅₀	1.3 nM Compound: S/GSK-1349572	Antiviral activity against Human immunodeficiency virus 1 3B harboring integrase S153Y/L101I/T124A/S153F mutant gene infected in human MT2 cells assessed as inhibition of virus induced cytopathic effect selected after 84 passages measured after 2 to 3 day Antiviral activity against Human immunodeficiency virus 1 3B harboring integrase S153Y/L101I/T124A/S153F mutant gene infected in human MT2 cells assessed as inhibition of virus induced cytopathic effect selected after 84 passages measured after 2 to 3 day	[PMID: 21115794]
MT2	EC₅₀	1.3 nM Compound: S/GSK-1349572	Antiviral activity against Human immunodeficiency virus 1 3B harboring integrase S153Y/L101I/T124A/S153F mutant gene infected in human MT2 cells assessed as inhibition of virus induced cytopathic effect selected after 98 passages measured after 2 to 3 day Antiviral activity against Human immunodeficiency virus 1 3B harboring integrase S153Y/L101I/T124A/S153F mutant gene infected in human MT2 cells assessed as inhibition of virus induced cytopathic effect selected after 98 passages measured after 2 to 3 day	[PMID: 21115794]
MT2	EC₅₀	1.3 nM Compound: S/GSK-1349572	Antiviral activity against Human immunodeficiency virus 1 3B harboring integrase S153Y/L101I/T124A/S153F mutant gene infected in human MT2 cells assessed as inhibition of virus induced cytopathic effect selected after 112 passages measured after 2 to 3 da Antiviral activity against Human immunodeficiency virus 1 3B harboring integrase S153Y/L101I/T124A/S153F mutant gene infected in human MT2 cells assessed as inhibition of virus induced cytopathic effect selected after 112 passages measured after 2 to 3 da	[PMID: 21115794]
MT4	EC₅₀	0.36 nM Compound: S/GSK-1349572	Antiviral activity against PI-resistant Human immunodeficiency virus 1 NL432 harboring nucleotide reverse transcriptase L24I/M46I/L63P/A71V/G73S/V82Tmutant infected in human MT4 cells after 2 to 3 days by reverse transcriptase activity Antiviral activity against PI-resistant Human immunodeficiency virus 1 NL432 harboring nucleotide reverse transcriptase L24I/M46I/L63P/A71V/G73S/V82Tmutant infected in human MT4 cells after 2 to 3 days by reverse transcriptase activity	[PMID: 21115794]
MT4	EC₅₀	0.71 nM Compound: S/GSK-1349572	Antiviral activity against Human immunodeficiency virus 1 3B infected in human MT4 cells assessed as viral viability after 4 to 5 days by Cell titer Glo luminescent assay Antiviral activity against Human immunodeficiency virus 1 3B infected in human MT4 cells assessed as viral viability after 4 to 5 days by Cell titer Glo luminescent assay	[PMID: 21115794]
MT4	CC₅₀	14 μM Compound: S/GSK-1349572	Cytotoxicity against human MT4 cells after 2 days by Cell titer Glo luminescent assay Cytotoxicity against human MT4 cells after 2 days by Cell titer Glo luminescent assay	[PMID: 21115794]
PBMC	CC₅₀	189 μM Compound: S/GSK-1349572	Cytotoxicity against PHA-stimulated human PBMC after 2 days by Cell titer Glo luminescent assay Cytotoxicity against PHA-stimulated human PBMC after 2 days by Cell titer Glo luminescent assay	[PMID: 21115794]
PBMC	CC₅₀	52 μM Compound: S/GSK-1349572	Cytotoxicity against unstimulated human PBMC after 2 days by Cell titer Glo luminescent assay Cytotoxicity against unstimulated human PBMC after 2 days by Cell titer Glo luminescent assay	[PMID: 21115794]
U-937	CC₅₀	7 μM Compound: S/GSK-1349572	Cytotoxicity against human U937 cells after 2 days by Cell titer Glo luminescent assay Cytotoxicity against human U937 cells after 2 days by Cell titer Glo luminescent assay	[PMID: 21115794]

体外研究
(In Vitro)

Dolutegravir (S/GSK1349572) 针对 PBMC 中 HIV-1 的 EC₅₀ 为 0.51 nM，在 MT-4 细胞中为 0.71 nM，在 PHIV 测定中为 2.2 nM，其使用假型自灭活病毒。Dolutegravir 在增殖的 IM-9、U-937、MT-4 和 Molt-4 细胞中的 50% 细胞毒性浓度 (CC₅₀) 分别为 4.8、7.0、14 和 15 μM。在未刺激和刺激的 PBMC 中，CC₅₀ 分别为 189 μM 和 52 μM。基于多替拉韦对 PBMC 中 HIV-1 的 EC₅₀ (即 0.51 nM)，这转化为基于细胞的治疗指数至少为9,400^[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

单次静脉内 (IV) 给药 Dolutegravir 后，血浆清除率在大鼠 (0.23 mL/min/kg) 和猴子 (2.12 mL/min/kg) 中较低。在大鼠和猴体内的半衰期相似，约为 6 小时，稳态分布容积 (V_SS) 较低。口服后，Dolutegravir 被快速吸收，当作为溶液给予禁食的雄性大鼠和一只猴子时具有高口服生物利用度 (分别为 75.6 和 87.0%)。Dolutegravir 暴露 (C_max 和 AUC) 随着剂量的增加而增加，在对非禁食大鼠和非禁食猴子口服给药高达 250 mg/kg 和高达 50 mg/kg 的悬浮液后，尽管增加小于比例^[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

441.36

Formula

C₂₀H₁₈F₂N₃NaO₅

CAS 号

1051375-19-9

性状

固体

颜色

Off-white to yellow

中文名称

度鲁特韦钠盐

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

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

溶解性数据

细胞实验：

DMSO 中的溶解度 : 2 mg/mL (4.53 mM; 超声助溶 (<60°C); 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

H₂O 中的溶解度 : < 0.1 mg/mL (insoluble)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.2657 mL	11.3286 mL	22.6572 mL
5 mM	---	---	---
10 mM	---	---	---

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* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

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Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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纯度 & 产品资料

纯度: 99.97%

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Data Sheet (629 KB) SDS (398 KB)

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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. [Content Brief]

[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. [Content Brief]

[3]. Hare S, et al. Structural and functional analyses of the second-generation integrase strand transfer inhibitor dolutegravir (S/GSK1349572). Mol Pharmacol. 2011 Oct;80(4):565-72. [Content Brief]

Cell Assay ^[1]	In vitro growth inhibition (cytotoxicity) studies are conducted with S/GSK1349572 (0.16, 0.8, 4, and 20 nM) in proliferating human leukemic and lymphomic cell lines (IM-9, U-937, MT-4, and Molt-4) as well as in stimulated and unstimulated human PBMCs. ATP levels are quantified by using the CellTiter-Glo luciferase reagent to measure the ability of a compound to inhibit cell growth as an indicator of the compound's potential for cytotoxicity^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[2]	For rat and monkey PK studies, Dolutegravir is administered as the free acid or the sodium salt. All doses are presented in terms of the free acid. Dolutegravir is administered by intravenous (IV) short-term (within 2 min) bolus (1 mg/kg) to three male rats and two male monkeys. For single oral administration, Dolutegravir as a solution (5 mg/kg) is administered to three fasted male rats and two fasted male monkeys. Dolutegravir is administered as single oral doses of 5, 50, 100, and 250 mg/kg to non-fasted male rats (n=2/dose level) and 3, 10, and 50 mg/kg to non-fasted female monkeys. For intravenous administration, blood samples are collected from rats (0.2 mL via jugular vein cannula) and monkeys (approximately 0.2 or 0.5 mL via saphenous vein in a hindlimb) into Na₂EDTA-treated syringes at 0.083, 0.25, 0.5, 1, 2, 4, 6, 8, and 24 h. For oral administration, samples are collected at 0.25 (rats only), 0.5, 1, 2, 4, 6 [rats (solution and suspension) and monkey (solution only)], 8, and 24 h. Following collection, the blood is immediately put on wet ice and then centrifuged within an hour at 1740 g for 10 min at 4°C to obtain plasma. All samples are stored at approximately -20°C or colder prior to analysis by using a method based on protein precipitation and LC-MS/MS analysis. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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. [Content Brief] [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. [Content Brief] [3]. Hare S, et al. Structural and functional analyses of the second-generation integrase strand transfer inhibitor dolutegravir (S/GSK1349572). Mol Pharmacol. 2011 Oct;80(4):565-72. [Content Brief]

Dolutegravir sodium 相关分类

Infection

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

DMSO

1 mM

2.2657 mL

11.3286 mL

22.6572 mL

56.6431 mL

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Keywords:

Dolutegravir1051375-19-9S/GSK1349572度鲁特韦钠盐HIV IntegraseHIVHuman immunodeficiency virusInhibitorinhibitorinhibit

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

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MCE 顾客使用本产品发表的 24 篇科研文献

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

Customer Review

Other Forms of Dolutegravir sodium:

Dolutegravir sodium 相关抗体

MCE 顾客使用本产品发表的 24 篇科研文献

Dolutegravir sodium 相关产品

•相关化合物库:

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查看 HIV 亚型特异性产品:

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参考文献

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