Cat. No.: HY-13238

Dolutegravir

(Synonyms: S/GSK1349572)

35 Cited Publications

Avis client

Based on 35 publication(s) in Google Scholar

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).

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Pureté: 99.94%
CAS No.: 1051375-16-6
Formule: C₂₀H₁₉F₂N₃O₅
Masse moléculaire:419.38

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months

Dolutegravir Chemical Structure

CAS No.: 1051375-16-6

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Essai clinique
Chemical Information
Publications (35)
Solvant et solubilité
- In Vitro
- In Vivo
Protocole
Pureté et documentation
Références
Help & FAQs
Bioz

Activité biologique

Description

IC₅₀ & Target

HIV-1

Voir tous les produits spécifiques à Isoform HIV :

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	IC₅₀	>100 μM Compound: DTG, S/GSK1349572, Dolutegravir	Inhibition of human OATP1B1 expressed in CHO cells using [3H]estradiol 17beta-D-glucuronide as substrate by liquid scintillation counting analysis Inhibition of human OATP1B1 expressed in CHO cells using [3H]estradiol 17beta-D-glucuronide as substrate by liquid scintillation counting analysis	[PMID: 23132334]
HEK293	IC₅₀	>100 μM Compound: DTG, S/GSK1349572, Dolutegravir	Inhibition of human OATP1B3 expressed in BacMam baculovirus virus infected HEK MSR2 cells using [3H]estradiol 17beta-D-glucuronide as substrate by liquid scintillation counting analysis Inhibition of human OATP1B3 expressed in BacMam baculovirus virus infected HEK MSR2 cells using [3H]estradiol 17beta-D-glucuronide as substrate by liquid scintillation counting analysis	[PMID: 23132334]
HEK-293T	IC₅₀	1.7 nM Compound: 3, DTG, S/GSK572, S/GSK1349572, Dolutegravir	Antiviral activity against pseudo Human immunodeficiency virus infected in HEK293T cells after 2 days Antiviral activity against pseudo Human immunodeficiency virus infected in HEK293T cells after 2 days	[PMID: 23845180]
HEK-293T	IC₅₀	22 nM Compound: 3, DTG, S/GSK572, S/GSK1349572, Dolutegravir	Antiviral activity against pseudo Human immunodeficiency virus infected in HEK293T cells after 2 days in presence of human serum albumin Antiviral activity against pseudo Human immunodeficiency virus infected in HEK293T cells after 2 days in presence of human serum albumin	[PMID: 23845180]
HOS	EC₅₀	1.6 nM Compound: 2, DTG	Antiviral activity against HIV-1 harboring wild type integrase infected in human HOS cells pretreated with compound for 3 hrs by single-round HIV-1 infectivity assay Antiviral activity against HIV-1 harboring wild type integrase infected in human HOS cells pretreated with compound for 3 hrs by single-round HIV-1 infectivity assay	[PMID: 24901667]
HOS	EC₅₀	11 nM Compound: 2, DTG	Antiviral activity against INSTI-resistant HIV-1 harboring integrase R263K mutant infected in human HOS cells pretreated with compound for 3 hrs by single-round HIV-1 infectivity assay Antiviral activity against INSTI-resistant HIV-1 harboring integrase R263K mutant infected in human HOS cells pretreated with compound for 3 hrs by single-round HIV-1 infectivity assay	[PMID: 24901667]
HOS	EC₅₀	13 nM Compound: 2, DTG	Antiviral activity against INSTI-resistant HIV-1 harboring integrase G118R mutant infected in human HOS cells pretreated with compound for 3 hrs by single-round HIV-1 infectivity assay Antiviral activity against INSTI-resistant HIV-1 harboring integrase G118R mutant infected in human HOS cells pretreated with compound for 3 hrs by single-round HIV-1 infectivity assay	[PMID: 24901667]
HOS	EC₅₀	3.6 nM Compound: 2, DTG	Antiviral activity against raltegravir-resistant HIV-1 harboring integrase N155H mutant infected in human HOS cells pretreated with compound for 3 hrs by single-round HIV-1 infectivity assay Antiviral activity against raltegravir-resistant HIV-1 harboring integrase N155H mutant infected in human HOS cells pretreated with compound for 3 hrs by single-round HIV-1 infectivity assay	[PMID: 24901667]
HOS	EC₅₀	4.3 nM Compound: 2, DTG	Antiviral activity against raltegravir-resistant HIV-1 harboring integrase Y143R mutant infected in human HOS cells pretreated with compound for 3 hrs by single-round HIV-1 infectivity assay Antiviral activity against raltegravir-resistant HIV-1 harboring integrase Y143R mutant infected in human HOS cells pretreated with compound for 3 hrs by single-round HIV-1 infectivity assay	[PMID: 24901667]
HOS	EC₅₀	5.8 nM Compound: 2, DTG	Antiviral activity against raltegravir-resistant HIV-1 harboring integrase G140S/Q148H double mutant infected in human HOS cells pretreated with compound for 3 hrs by single-round HIV-1 infectivity assay Antiviral activity against raltegravir-resistant HIV-1 harboring integrase G140S/Q148H double mutant infected in human HOS cells pretreated with compound for 3 hrs by single-round HIV-1 infectivity assay	[PMID: 24901667]
MDCK-II	IC₅₀	>100 μM Compound: DTG, S/GSK1349572, Dolutegravir	Inhibition of MDR1 (unknown origin) expressed in MDCK2 cells assessed as basolateral to apical transport of [3H]digoxin after 90 mins by liquid scintillation counting analysis Inhibition of MDR1 (unknown origin) expressed in MDCK2 cells assessed as basolateral to apical transport of [3H]digoxin after 90 mins by liquid scintillation counting analysis	[PMID: 23132334]
MDCK-II	IC₅₀	>30 μM Compound: DTG, S/GSK1349572, Dolutegravir	Inhibition of BCRP (unknown origin) expressed in MDCK2 cells assessed as basolateral to apical transport of [14C]cimetidine after 90 mins by liquid scintillation counting analysis Inhibition of BCRP (unknown origin) expressed in MDCK2 cells assessed as basolateral to apical transport of [14C]cimetidine after 90 mins by liquid scintillation counting analysis	[PMID: 23132334]
MDCK-II	IC₅₀	1.9 μM Compound: DTG, S/GSK1349572, Dolutegravir	Inhibition of human OCT2 expressed in MDCK2 cells using [14C]metformin as substrate by liquid scintillation counting analysis Inhibition of human OCT2 expressed in MDCK2 cells using [14C]metformin as substrate by liquid scintillation counting analysis	[PMID: 23132334]
MT4	IC₅₀	2 nM Compound: 3, DTG, S/GSK572, S/GSK1349572, Dolutegravir	Antiviral activity against Human immunodeficiency virus 1 3B infected in human MT4 cells after 4 to 5 days by bioluminescence assay Antiviral activity against Human immunodeficiency virus 1 3B infected in human MT4 cells after 4 to 5 days by bioluminescence assay	[PMID: 23845180]
Sf9	IC₅₀	>100 μM Compound: DTG, S/GSK1349572, Dolutegravir	Inhibition of human MRP2 expressed in baculovirus-infected Sf9 cell membrane vesicle using [3H]estradiol 17beta-D-glucuronide as substrate preincubated with vesicles for 5 mins prior to substrate addition by liquid scintillation counting analysis Inhibition of human MRP2 expressed in baculovirus-infected Sf9 cell membrane vesicle using [3H]estradiol 17beta-D-glucuronide as substrate preincubated with vesicles for 5 mins prior to substrate addition by liquid scintillation counting analysis	[PMID: 23132334]
Vero C1008	CC₅₀	>40 μM Compound: Dolutegravir	Cytotoxicity (CC50) determination in Vero E6 cells measured by fluorescence (OD590nm) Cytotoxicity (CC50) determination in Vero E6 cells measured by fluorescence (OD590nm)	10.1101/2020.04.03.023846
Vero C1008	EC₅₀	22.04 μM Compound: Dolutegravir	Antiviral efficacy against SARS-CoV-2 (strain BavPat1) in Vero E6 cells assessed by inhibition of viral RNA replication measured by RT-PCR after 2 days Antiviral efficacy against SARS-CoV-2 (strain BavPat1) in Vero E6 cells assessed by inhibition of viral RNA replication measured by RT-PCR after 2 days	10.1101/2020.04.03.023846

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^[3].

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

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 1051375-16-6
Appearance Solid
Masse moléculaire 419.38
Formule C₂₀H₁₉F₂N₃O₅
Color White to off-white
SMILES

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

S/GSK1349572
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

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

Publications (35)

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Journal Impact Factor

Science

Structural basis of second-generation HIV integrase inhibitor action and viral resistance. [Abstract]

2020 Feb 14;367(6479):806-810. PMID: 32001525
Cell

Combination antiretroviral therapy and MCL-1 inhibition mitigate HTLV-1 infection in vivo. [Abstract]

2025 Sep 4;188(18):4896-4912.e19. PMID: 40645177
Sci Adv

Elucidating the mechanism by which HIV-1 nucleocapsid mutations confer resistance to integrase strand transfer inhibitors. [Abstract]

2025 Sep 12;11(37):eadz8980. PMID: 40938996

Dolutegravir purchased from MedChemExpress. Usage Cited in: Sci Adv. 2025 Sep 12;11(37):eadz8980. [Abstract]

Replication kinetics of the indicated NL4-3 variants of HIV-1 in the SupT1 T cell line in the absence or presence of Dolutegravir (DTG) (1-10 nM).
Cell Rep Med

Decoupling HIV-1 antiretroviral drug inhibition from plasma antibody activity to evaluate broadly neutralizing antibody therapeutics and vaccines. [Abstract]

2024 Aug 26:101702. PMID: 39216479
Cell Rep Med

Combination of compound screening with an animal model identifies pentamidine to prevent Chlamydia trachomatis infection. [Abstract]

2024 Jul 2:101643. PMID: 38981484

Dolutegravir purchased from MedChemExpress. Usage Cited in: Cell Rep Med. 2024 Jul 2:101643. [Abstract]

Dose-response curves for Dolutegravir (0.5-13.5 μM) against Ct serovars E, F, and L2. POC represented the percentage of DMSO-treated control.

Dolutegravir purchased from MedChemExpress. Usage Cited in: Cell Rep Med. 2024 Jul 2:101643. [Abstract]

Dolutegravir (13.5 μM) significantly blocked Ct growth in mice for genital chlamydia infection.
Biomed Pharmacother

Differential adipose tissue remodeling and metabolic effects of dolutegravir and bictegravir: implications for HIV therapy. [Abstract]

2025 Nov 28:193:118831. PMID: 41317481
Biochem Pharmacol

Divergent effects of the antiretroviral drugs, dolutegravir, tenofovir alafenamide, and tenofovir disoproxil fumarate, on human adipocyte function. [Abstract]

2024 Feb:220:116010. PMID: 38154544

Dolutegravir purchased from MedChemExpress. Usage Cited in: Biochem Pharmacol. 2024 Feb:220:116010. [Abstract]

10 μM Dolutegravir (DTG) (1-10 μM) significantly repressed the mRNA expression levels of the adipocyte identity markers, peroxisome proliferator-activated receptor-gamma (PPARG) and lipoprotein lipase (LPL), as well as solute carrier family 2, facilitated glucose transporter member 4 (SLC2A4, GLUT4), and the adipokine, adiponectin (ADIPOQ), but induced that of solute carrier family 2, facilitated glucose transporter member 1 (SLC2A1, GLUT1) and leptin (LEP) in SGBS human adipocytes.

Dolutegravir purchased from MedChemExpress. Usage Cited in: Biochem Pharmacol. 2024 Feb:220:116010. [Abstract]

The effects of Dolutegravir (DTG) (1-10 μM) on the releases of leptin and adiponectin to the cell culture medium of differentiating SGBS human adipocytes are shown.
Life Sci

Differential effects of dolutegravir, bictegravir and raltegravir in adipokines and inflammation markers on human adipocytes. [Abstract]

2022 Nov 1:308:120948. PMID: 36096241
Pharmaceuticals (Basel)

Evaluation of the Potency of Anti-HIV and Anti-HCV Drugs to Inhibit P-Glycoprotein Mediated Efflux of Digoxin in Caco-2 Cell Line and Human Precision-Cut Intestinal Slices. [Abstract]

2022 Feb 18;15(2):242. PMID: 35215354
Int J Antimicrob Agents

Efficacy of antiretroviral compounds against Toxoplasma gondii in vitro. [Abstract]

2019 Dec;54(6):814-819. PMID: 31479744
J Infect Dis

Second-generation HIV integrase inhibitors induce differentiation dysregulation and exert toxic effects in human embryonic stem cell and mouse models. [Abstract]

2022 Nov 28;226(11):1992-2001. PMID: 36124861
FASEB J

Dolutegravir induces endoplasmic reticulum stress at the blood-brain barrier. [Abstract]

2025 Feb 28;39(4):e70377. PMID: 39985305
Antiviral Res

Differential effects of antiretroviral HIV integrase inhibitors on vascular cell adhesion molecules. [Abstract]

2025 Sep 11:106283. PMID: 40945692
Drug Metab Dispos

A Systematic In Vitro Investigation of the Inhibitor Preincubation Effect on Multiple Classes of Clinically Relevant Transporters. [Abstract]

2019 Jul;47(7):768-778. PMID: 31068368
Drug Metab Dispos

Mechanistic Assessment of Extrahepatic Contributions to Glucuronidation of Integrase Strand Transfer Inhibitors. [Abstract]

2019 May;47(5):535-544. PMID: 30804050
Open Forum Infect Dis

Novel Dolutegravir and Lenacapavir Resistance Patterns in Human Immunodeficiency Virus Type 2 Infection: A Case Report. [Abstract]

2024 Nov 29;12(1):ofae705. PMID: 39741997
Anal Bioanal Chem

Development and validation of an LC-MS/MS assay for the quantification of dolutegravir extracted from human hair. [Abstract]

2018 Nov;410(29):7773-7781. PMID: 30280227
ASN Neuro

Exposure to Frontline Antiretroviral Dolutegravir Disrupts Oligodendrocyte Development Across Differentiation Stages. [Abstract]

2026;18(1):2647877. PMID: 41904696
J Antimicrob Chemother

Cooperation between HIV-1 integrase natural polymorphism K156N and 3'PPT mutations in dolutegravir monotherapy failure. [Abstract]

2026 Feb 2;81(3):dkag033. PMID: 41636646
Viruses

Efficacy of Integrase Strand Transfer Inhibitors and the Capsid Inhibitor Lenacapavir against HIV-2, and Exploring the Effect of Raltegravir on the Activity of SARS-CoV-2. [Abstract]

2024 Oct 13;16(10):1607. PMID: 39459940
Viruses

Analysis and Molecular Determinants of HIV RNase H Cleavage Specificity at the PPT/U3 Junction. [Abstract]

2021 Jan 18;13(1):131. PMID: 33477685
J Neuroimmune Pharmacol

Antiretroviral Drugs Promote Amyloidogenesis by De-Acidifying Endolysosomes. [Abstract]

2021 Mar;16(1):159-168. PMID: 31338753
Toxicol Appl Pharmacol

The inhibitory effect of antiretroviral drugs on the L-carnitine uptake in human placenta. [Abstract]

2019 Apr 1:368:18-25. PMID: 30735677
PLoS One

HIV antiretroviral drugs, dolutegravir, maraviroc and ritonavir-boosted atazanavir use different pathways to affect inflammation, senescence and insulin sensitivity in human coronary endothelial cells. [Abstract]

2020 Jan 23;15(1):e0226924. PMID: 31971958
J Clin Pharmacol

Characterization of the Ontogeny of Hepatic UDP-Glucuronosyltransferase Enzymes Based on Glucuronidation Activity Measured in Human Liver Microsomes. [Abstract]

2019 Sep;59 Suppl 1:S42-S55. PMID: 31502688
Antivir Ther

Impact of CCR5, integrase and protease inhibitors on human endothelial cell function, stress, inflammation and senescence. [Abstract]

2017;22(8):645-657. PMID: 28350300

Dolutegravir 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%.
Biochem Biophys Res Commun

The inhibition process of HIV-1 integrase by diketoacids molecules: Understanding the factors governing the better efficiency of dolutegravir. [Abstract]

2017 Jul 1;488(3):433-438. PMID: 28478035
Cell Physiol Biochem

Enhanced Eryptosis Following Exposure to Dolutegravir. [Abstract]

2016 Jul 21;39(2):639-650. PMID: 27442249

Dolutegravir 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).
STAR Protoc

Protocol to generate microglia-containing cerebral organoids to model HIV neuroinflammation. [Abstract]

2026 Jun 19;7(2):104604. PMID: 42224077
bioRxiv

2026 Apr 21.
University of Debrecen

2023.
bioRxiv

Elucidating the Mechanism by Which HIV-1 Nucleocapsid Mutations Confer Resistance to Integrase Strand Transfer Inhibitors. [Abstract]

2025 May 18:2025.05.17.654662. PMID: 41030995
Res Sq

2024 May 24.
Preprints

2024 Apr 23.
PeerJ Physical Chemistry

2019, 1:e6.

Solvant et solubilité

In Vitro:

DMSO : 35 mg/mL (83.46 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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. 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 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

Protocol 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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 4

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.96 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protocole

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].

MedChemExpress (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.

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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

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COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
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MS (2659 KB)
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IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[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

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.3845 mL	11.9224 mL	23.8447 mL	59.6118 mL
	5 mM	0.4769 mL	2.3845 mL	4.7689 mL	11.9224 mL
	10 mM	0.2384 mL	1.1922 mL	2.3845 mL	5.9612 mL
	15 mM	0.1590 mL	0.7948 mL	1.5896 mL	3.9741 mL
	20 mM	0.1192 mL	0.5961 mL	1.1922 mL	2.9806 mL
	25 mM	0.0954 mL	0.4769 mL	0.9538 mL	2.3845 mL
	30 mM	0.0795 mL	0.3974 mL	0.7948 mL	1.9871 mL
	40 mM	0.0596 mL	0.2981 mL	0.5961 mL	1.4903 mL
	50 mM	0.0477 mL	0.2384 mL	0.4769 mL	1.1922 mL
	60 mM	0.0397 mL	0.1987 mL	0.3974 mL	0.9935 mL
	80 mM	0.0298 mL	0.1490 mL	0.2981 mL	0.7451 mL

Keywords

Dolutegravir

35 Cited Publications

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Dolutegravir

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Publications Citing Use of MedChemExpress (MCE) Dolutegravir

Voir tous les produits spécifiques à Isoform HIV

Activité biologique

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Publications (35)

Solvant et solubilité

Protocole

Pureté et documentation

Références

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Complete Stock Solution Preparation Table

Dolutegravir

Anti-Infection Compound Library

Metabolism/Protease Compound Library

FDA-Approved Drug Library

Antiviral Compound Library

Drug Repurposing Compound Library

Anti-COVID-19 Compound Library

Orally Active Compound Library

FDA Approved & Pharmacopeial Drug Library

Targeted Diversity Library

Rare Diseases Drug Library

Pediatric Drug Library

EMA-Approved Drug Library

Human Metabolite Library

Metabolic Enzyme Compound Library

Mitochondrial Toxicity Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

FDA-Approved Drug Library Mini

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Classic FDA-Approved Drug Library

Publications Citing Use of MedChemExpress (MCE) Dolutegravir

Voir tous les produits spécifiques à Isoform HIV

Activité biologique

Chemical Information

Publications (35)

Solvant et solubilité

Protocole

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Dolutegravir Related Classifications

Cat. No.: HY-13238