Dolutegravir sodium (Synonyms: S/GSK1349572 sodium)

Name: Dolutegravir sodium
Brand: MedChemExpress
SKU: HY-13238A
Rating: 5.0 (25 reviews)

Cat. No.: HY-13238A Purity: 99.97%: FAQs
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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).

For research use only. We do not sell to patients.

Dolutegravir sodium Chemical Structure

CAS No. : 1051375-19-9

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10 mM * 1 mL in DMSO	USD 99	In-stock	Estimated Time of Arrival: December 31
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5 mg	USD 90	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 140	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 350	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 500	In-stock	Estimated Time of Arrival: December 31
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Based on 25 publication(s) in Google Scholar

Other Forms of Dolutegravir sodium:

Dolutegravir In-stock

23 Publications Citing Use of MCE Dolutegravir sodium

Proliferation Assay

: Dolutegravir sodium purchased from MedChemExpress. 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 MedChemExpress. 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

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

HIV-1

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]

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^[1].

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

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^[2].

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

Clinical Trial

Molecular Weight

441.36

Formula

C₂₀H₁₈F₂N₃NaO₅

CAS No.

1051375-19-9

Appearance

Solid

Color

Off-white to yellow

SMILES

O=C(C1=CN(C2=C(O[Na])C1=O)C[C@]3([H])OCC[C@@H](C)N3C2=O)NCC4=CC=C(F)C=C4F

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

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

Solvent & Solubility

In Vitro:

DMSO : 2 mg/mL (4.53 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 1 mg/mL (2.27 mM; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: 99.97%

Select Batch:

Data Sheet (279 KB) SDS (398 KB)

COA (249 KB) HNMR (293 KB) LCMS (95 KB)

Handling Instructions (2659 KB)

References

[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.
References	[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]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

H₂O / DMSO

1 mM

2.2657 mL

11.3286 mL

22.6572 mL

56.6431 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Dolutegravir sodium Related Classifications

Infection

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Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Dolutegravir1051375-19-9S/GSK1349572HIV IntegraseHIVHuman immunodeficiency virusInhibitorinhibitorinhibit

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Dolutegravir sodium (Synonyms: S/GSK1349572 sodium)

Customer Review

Other Forms of Dolutegravir sodium:

Dolutegravir sodium Related Antibodies

23 Publications Citing Use of MCE Dolutegravir sodium

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•Related Screening Libraries:

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View All HIV Isoform Specific Products:

Biological Activity

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Purity & Documentation

References

Customer Review

Dolutegravir sodium Related Antibodies

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Complete Stock Solution Preparation Table

Dolutegravir sodium Related Classifications

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