Dolutegravir (Synonyms: S/GSK1349572)

Cat. No.: HY-13238 Purity: 99.65%: FAQs
Data Sheet SDS COA Handling Instructions

Dolutegravir (S/GSK1349572) 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 (S/GSK1349572) inhibits HIV-1 viral replication with an IC₅₀ of 0.51 nM in peripheral blood mononuclear cells. Dolutegravir 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 Chemical Structure

CAS No. : 1051375-16-6

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10 mM * 1 mL in DMSO	USD 81	In-stock	Estimated Time of Arrival: December 31
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10 mM * 1 mL ready for reconstitution	USD 81	In-stock	Estimated Time of Arrival: December 31
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5 mg	USD 88	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 154	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 385	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 605	In-stock	Estimated Time of Arrival: December 31
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500 mg	USD 1210	In-stock	Estimated Time of Arrival: December 31
1 g	USD 1595	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 19 publication(s) in Google Scholar

Other Forms of Dolutegravir:

Dolutegravir sodium In-stock
Cabotegravir In-stock

17 Publications Citing Use of MCE Dolutegravir

Proliferation Assay

: Dolutegravir 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 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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Description

IC₅₀ & Target

IC50: 2.7 nM (HIV-1 integrase-catalyzed strand transfer)^[1]

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].

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^[3].

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

Clinical Trial

Molecular Weight

419.38

Appearance

Solid

Formula

C₂₀H₁₉F₂N₃O₅

CAS No.

1051375-16-6

SMILES

FC1=CC(F)=C(C=C1)CNC(C2=CN(C3=C(C2=O)O)C[[email protected]@]([H])(N4C3=O)OCC[[email protected]]4C)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 10 mg/mL (23.84 mM; Need ultrasonic and warming)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.3845 mL	11.9224 mL	23.8447 mL
5 mM	0.4769 mL	2.3845 mL	4.7689 mL
10 mM	0.2384 mL	1.1922 mL	2.3845 mL

*Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 5% DMSO 95% (20% SBE-β-CD in saline)
Solubility: ≥ 2.62 mg/mL (6.25 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (5.96 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (5.96 mM); Clear solution
4.

Add each solvent one by one: 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (5.96 mM); Clear solution

*All of the co-solvents are available by MCE.

Purity & Documentation

Purity: 99.65%

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Data Sheet (280 KB) SDS (398 KB)

COA (248 KB) LCMS (267 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]. 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]

[3]. 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]

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]. 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] [3]. 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]

Help & FAQs

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.

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Keywords:

Dolutegravir1051375-16-6S/GSK1349572HIV IntegraseHIVHuman immunodeficiency virusInhibitorinhibitorinhibit

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Dolutegravir (Synonyms: S/GSK1349572)

Customer Review

Other Forms of Dolutegravir:

17 Publications Citing Use of MCE Dolutegravir

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•Related Screening Libraries:

Biological Activity

Protocol

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