1. Metabolic Enzyme/Protease
    Anti-infection
  2. HIV Integrase
    HIV

Dolutegravir (Synonyms: S/GSK1349572; GSK1349572; S/GSK 1349572; GSK-1349572; GSK 1349572)

Cat. No.: HY-13238 Purity: 99.54%
Data Sheet SDS Handling Instructions

Dolutegravir is an inhibitor of HIV-1 integrase-catalyzed strand transfer with IC50 of 2.7 nM.

For research use only. We do not sell to patients.
Dolutegravir Chemical Structure

Dolutegravir Chemical Structure

CAS No. : 1051375-16-6

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Description

Dolutegravir is an inhibitor of HIV-1 integrase-catalyzed strand transfer with IC50 of 2.7 nM.

IC50 & Target

IC50: 2.7 nM (HIV-1 integrase)[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].

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 (VSS) 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 (Cmax 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].

Clinical Trial
NCT Number Sponsor Condition Start Date Phase
NCT01068925 GlaxoSmithKline|Shionogi HIV Infections February 2010 Phase 1
NCT01098513 ViiV Healthcare|GlaxoSmithKline Infection, Human Immunodeficiency Virus April 2010 Phase 1
NCT01098526 GlaxoSmithKline|Shionogi Infections, Human Immunodeficiency Virus and Herpesviridae|Healthy March 2010 Phase 1
NCT00631592 ViiV Healthcare Healthy Subjects February 2008 Phase 1
NCT00774111 GlaxoSmithKline|Shionogi Healthy Subjects October 2008 Phase 1
NCT01459315 University of North Carolina, Chapel Hill|GlaxoSmithKline Healthy November 2011 Phase 1
NCT00726336 GlaxoSmithKline Healthy Subjects August 2008 Phase 1
NCT01209065 ViiV Healthcare|GlaxoSmithKline Infections, Human Immunodeficiency Virus and Herpesviridae September 2010 Phase 1
NCT00950859 ViiV Healthcare|GlaxoSmithKline Infection, Human Immunodeficiency Virus August 2009 Phase 2
NCT01231529 ViiV Healthcare|Shionogi|GlaxoSmithKline Healthy Subjects|Hepatic Impairment|Infection, Human Immunodeficiency Virus November 2010 Phase 1
NCT00555035 GlaxoSmithKline Healthy Subjects November 2007 Phase 1
NCT02401828 Erasmus Medical Center Human Immunodeficiency Virus March 2015 Phase 4
NCT01404806 University of North Carolina, Chapel Hill|GlaxoSmithKline Healthy Adult Females August 2011 Phase 1
NCT00774735 GlaxoSmithKline|Shionogi Healthy Subjects|Infection, Human Immunodeficiency Virus October 2008 Phase 1
NCT00883935 GlaxoSmithKline|Shionogi Healthy Volunteer April 2009 Phase 1
NCT00996021 GlaxoSmithKline|Shionogi Healthy Subjects September 2009 Phase 1
NCT00828763 GlaxoSmithKline|Shionogi Healthy Volunteer February 2009 Phase 1
NCT00867152 ViiV Healthcare|Shionogi Healthy Volunteer April 2009 Phase 1
NCT02487706 Fundacio Lluita Contra la SIDA HIV June 2015 Phase 4
NCT00858455 GlaxoSmithKline|Shionogi Healthy Volunteer January 2009 Phase 1
NCT00708110 ViiV Healthcare|Shionogi|GlaxoSmithKline Infection, Human Immunodeficiency Virus June 2008 Phase 2
NCT01231542 ViiV Healthcare|Shionogi|GlaxoSmithKline Infection, Human Immunodeficiency Virus May 2011 Phase 1
NCT01568892 ViiV Healthcare|Shionogi|GlaxoSmithKline Infection, Human Immunodeficiency Virus April 2012 Phase 3
NCT01227824 ViiV Healthcare|Shionogi|GlaxoSmithKline Infection, Human Immunodeficiency Virus I October 2010 Phase 3
NCT01231516 ViiV Healthcare|Shionogi|GlaxoSmithKline Infection, Human Immunodeficiency Virus October 2010 Phase 3
NCT01498861 ViiV Healthcare|Shionogi|GlaxoSmithKline Infection, Human Immunodeficiency Virus December 2011 Phase 1
NCT01353716 ViiV Healthcare|Shionogi|GlaxoSmithKline Infection, Human Immunodeficiency Virus June 2011 Phase 1
NCT00951015 ViiV Healthcare|Shionogi|GlaxoSmithKline Infection, Human Immunodeficiency Virus July 30, 2009 Phase 2
NCT01214993 ViiV Healthcare|Shionogi|GlaxoSmithKline Infections, Human Immunodeficiency Virus and Tuberculosis October 2010 Phase 1
NCT02500446 University of Melbourne|The Alfred|ViiV Healthcare HIV September 28, 2015 Phase 4
NCT01332565 ViiV Healthcare|Shionogi|GlaxoSmithKline Infection, Human Immunodeficiency Virus April 2011 Phase 1
NCT02098837 St Stephens Aids Trust HIV April 2014 Phase 4
NCT03016533 ViiV Healthcare|PPD Infection, Human Immunodeficiency Virus August 1, 2017 Phase 3
NCT02924389 Emory University|National Institutes of Health (NIH) HIV September 2016
NCT01425099 ViiV Healthcare|Shionogi|GlaxoSmithKline Infection, Human Immunodeficiency Virus September 2011 Phase 1
NCT02491242 Asociacion para el Estudio de las Enfermedades Infecciosas HIV Infection November 2015
NCT02245022 University of Liverpool|ViiV Healthcare|Makerere University HIV|Pregnancy March 14, 2017 Phase 2|Phase 3
NCT00942136 GlaxoSmithKline|Shionogi Healthy Volunteer July 2009 Phase 1
NCT01467531 ViiV Healthcare|Shionogi Infections, Human Immunodeficiency Virus and Hepatitis November 2011 Phase 1
NCT02572947 Calmy Alexandra|University Hospital, Geneva Human Immunodeficiency Virus|Dolutegravir|Monotherapy|Treatment Efficacy June 2016 Phase 2
NCT02285374 St Stephens Aids Trust|ViiV Healthcare HIV November 2014 Phase 4
NCT01467518 ViiV Healthcare|Shionogi|GlaxoSmithKline Infections, Human Immunodeficiency Virus and Hepatitis December 2011 Phase 1
NCT01263015 ViiV Healthcare|Shionogi|GlaxoSmithKline Infection, Human Immunodeficiency Virus I February 2011 Phase 3
NCT01499199 ViiV Healthcare|Shionogi|GlaxoSmithKline Infection, Human Immunodeficiency Virus January 2012 Phase 3
NCT01328041 ViiV Healthcare|Shionogi|GlaxoSmithKline Infection, Human Immunodeficiency Virus May 2011 Phase 3
NCT02211482 The Huesped Foundation|ViiV Healthcare HIV-1 Infection October 2014 Phase 4
NCT02551523 University of Zurich Monotherapy|Dolutegravir|Primary HIV Infection|Treatment Efficacy November 2015 Phase 2
NCT03094507 St Stephens Aids Trust|ViiV Healthcare HIV April 19, 2017 Phase 1
NCT02596334 Centre Hospitalier Régional d'Orléans HIV December 23, 2015 Phase 3
NCT02509195 St Stephens Aids Trust|ViiV Healthcare HIV July 2015 Phase 4
NCT02976259 Institut de Médecine et d'Epidémiologie Appliquée - Fondation Internationale Léon M'Ba HIV Infection Primary December 2016 Phase 3
NCT02218320 University of North Carolina, Chapel Hill|Merck Sharp & Dohme Corp. Human Immunodeficiency Virus October 2014 Phase 4
NCT02404805 University of Colorado, Denver HIV|Hepatitis C February 2016
NCT02566707 Radboud University HIV-1 Infection August 2015 Phase 2
NCT02263326 Babafemi Taiwo|ViiV Healthcare|Northwestern University HIV Infection December 2014 Phase 3
NCT01283100 ViiV Healthcare|GlaxoSmithKline Infection, Human Immunodeficiency Virus I March 2011 Phase 1
NCT01382238 ViiV Healthcare|Shionogi|GlaxoSmithKline Infections, Human Immunodeficiency Virus and Herpesviridae June 2011 Phase 1
NCT02242799 University of Liverpool|ViiV Healthcare|Makerere University Malaria|HIV June 2015 Phase 1
NCT01966822 Fundacio Lluita Contra la SIDA HIV-1 Infection January 2014 Phase 3
NCT02076386 ViiV Healthcare|GlaxoSmithKline Infection, Human Immunodeficiency Virus March 4, 2014
NCT02499978 Stanford University|Janssen Scientific Affairs, LLC|University of Colorado, Denver HIV/AIDS May 2016 Phase 2|Phase 3
NCT02527096 French National Institute for Health and Medical Research-French National Agency for Research on AIDS and Viral Hepatitis (Inserm-ANRS)|ViiV Healthcare HIV-1 Infection September 2015 Phase 2
NCT03033836 The Huesped Foundation|ViiV Healthcare HIV Infections December 2015 Phase 4
NCT02542852 Castagna Antonella|Bristol-Myers Squibb|ViiV Healthcare|Ospedale San Raffaele HIV-1 Infection September 2015 Phase 2
NCT02185300 ViiV Healthcare|GlaxoSmithKline Infection, Human Immunodeficiency Virus July 2014 Phase 1
NCT02211690 Andrew Carr|ViiV Healthcare Australia Pty. Ltd|St Vincent's Hospital, Sydney Human Immunodeficiency Virus August 2014 Phase 4
NCT02656511 University of California, San Francisco|ViiV Healthcare|Gilead Sciences HIV December 2015 Phase 4
NCT01366547 ViiV Healthcare|Shionogi|GlaxoSmithKline Healthy Subjects|Infection, Human Immunodeficiency Virus June 2011 Phase 1
NCT02067767 Nantes University Hospital HIV-1 Infection February 2014 Phase 2
NCT03017872 Kirby Institute|UNITAID|National Health and Medical Research Council, Australia|ViiV Healthcare|Janssen Pharmaceutica HIV Infections July 2017 Phase 4
NCT01827540 Tobira Therapeutics, Inc.|ViiV Healthcare HIV-infection/AIDS March 2013 Phase 1
NCT02659761 University College Dublin|Mater Misericordiae University Hospital|ViiV Healthcare Human Immunodeficiency Virus November 2016 Phase 4
NCT02064374 ViiV Healthcare|GlaxoSmithKline Infection, Human Immunodeficiency Virus February 2014 Phase 1
NCT01449929 ViiV Healthcare|GlaxoSmithKline Infection, Human Immunodeficiency Virus October 2011 Phase 3
NCT02715479 ViiV Healthcare|GlaxoSmithKline Infection, Human Immunodeficiency Virus April 2016 Phase 1
NCT01762995 ViiV Healthcare|GlaxoSmithKline Infection, Human Immunodeficiency Virus December 2012 Phase 1
NCT02069834 Nantes University Hospital HIV Infection|HAART-treated|Virologically Controlled May 2014 Phase 2|Phase 3
NCT02777229 French National Institute for Health and Medical Research-French National Agency for Research on AIDS and Viral Hepatitis (Inserm-ANRS)|Institut de Recherche pour le Developpement HIV-1 Infection July 2016 Phase 3
NCT02337322 Juan A. Arnaiz|Hospital Clinic of Barcelona Acquired Immune Deficiency Syndrome Virus April 2015 Phase 4
NCT02219217 St Stephens Aids Trust|ViiV Healthcare HIV October 2014 Phase 1
NCT01622790 ViiV Healthcare|Shionogi|GlaxoSmithKline Infection, Human Immunodeficiency Virus June 2012 Phase 1
NCT02893488 ViiV Healthcare Infection, Human Immunodeficiency Virus September 2016 Phase 1
NCT02370979 University Hospital, Strasbourg, France HIV-1 Infection February 2015 Phase 4
NCT02513147 Hospital Universitari Vall d'Hebron Research Institute|University Hospital, Ghent|IrsiCaixa HIV-1 June 2015 Phase 4
NCT02384395 University of North Carolina, Chapel Hill|ViiV Healthcare|National Cancer Institute (NCI) HIV|Acute HIV Infection September 2015
NCT02738931 ViiV Healthcare|GlaxoSmithKline Infection, Human Immunodeficiency Virus May 2016 Phase 1
NCT03095638 ViiV Healthcare|GlaxoSmithKline Infection, Human Immunodeficiency Virus May 1, 2017 Phase 1
NCT02582684 AIDS Clinical Trials Group|National Institute of Allergy and Infectious Diseases (NIAID) HIV-1 Infection December 2015 Phase 2
NCT01563328 ViiV Healthcare|Shionogi|GlaxoSmithKline Infection, Human Immunodeficiency Virus March 1, 2012 Phase 1
NCT01536873 ViiV Healthcare|GlaxoSmithKline Infection, Human Immunodeficiency Virus June 2012 Phase 3
NCT02486133 Technische Universität München HIV-Infection July 2015 Phase 3
NCT02987530 French National Institute for Health and Medical Research-French National Agency for Research on AIDS and Viral Hepatitis (Inserm-ANRS)|Institut National de la Santé Et de la Recherche Médicale, France HIV-1 Infection January 2017 Phase 3
NCT03078556 ViiV Healthcare|GlaxoSmithKline Infection, Human Immunodeficiency Virus March 27, 2017 Phase 1
NCT02878642 University Hospital, Caen HIV May 2015
NCT02397694 Gilead Sciences HIV-1 Infection March 2015 Phase 2
NCT01302847 National Institute of Allergy and Infectious Diseases (NIAID) HIV Infections March 2011 Phase 1|Phase 2
NCT02831673 ViiV Healthcare|PPD|GlaxoSmithKline Infection, Human Immunodeficiency Virus July 21, 2016 Phase 3
NCT02178592 ViiV Healthcare|GlaxoSmithKline Infection, Human Immunodeficiency Virus January 1, 2015 Phase 3
NCT02373930 ViiV Healthcare|Janssen Pharmaceuticals|GlaxoSmithKline Infection, Human Immunodeficiency Virus February 2015 Phase 1
NCT02105987 ViiV Healthcare|PPD|GlaxoSmithKline Infection, Human Immunodeficiency Virus April 2014 Phase 3
NCT02831764 ViiV Healthcare|GlaxoSmithKline Infection, Human Immunodeficiency Virus July 18, 2016 Phase 3
NCT01896921 University of Maryland HIV September 2013 Phase 3
NCT02741557 ViiV Healthcare|GlaxoSmithKline Infection, Human Immunodeficiency Virus May 2016 Phase 1
NCT02882230 Fondation Ophtalmologique Adolphe de Rothschild HIV September 2016
NCT01967771 ViiV Healthcare|GlaxoSmithKline Infection, Human Immunodeficiency Virus October 2013 Phase 1
NCT02429791 ViiV Healthcare|Janssen, GlaxoSmithKline (GSK) Infection, Human Immunodeficiency Virus April 2015 Phase 3
NCT02422797 ViiV Healthcare|Janssen Pharmaceuticals|GlaxoSmithKline Infection, Human Immunodeficiency Virus April 21, 2015 Phase 3
NCT02557997 University Hospital, Strasbourg, France HIV-1 Infection April 2014
NCT02771249 National Institutes of Health Clinical Center (CC) Healthy Volunteers May 5, 2016 Phase 1
NCT02539576 ViiV Healthcare|GlaxoSmithKline Infection, Human Immunodeficiency Virus October 2015 Phase 1
NCT02603120 Gilead Sciences HIV-1 Infection November 11, 2015 Phase 3
NCT02478632 ViiV Healthcare|Janssen, GlaxoSmithKline (GSK) Infection, Human Immunodeficiency Virus June 1, 2015 Phase 3
NCT03122262 Willem Daniel Francois Venter|University of Witwatersrand, South Africa HIV-1 Infection January 2017 Phase 3
NCT03048422 National Institute of Allergy and Infectious Diseases (NIAID) HIV Infections July 1, 2017 Phase 3
NCT02227238 ViiV Healthcare|GlaxoSmithKline Infection, Human Immunodeficiency Virus December 1, 2014 Phase 3
NCT01910402 ViiV Healthcare|GlaxoSmithKline Infection, Human Immunodeficiency Virus August 1, 2013 Phase 3
NCT02607956 Gilead Sciences HIV-1 Infection November 11, 2015 Phase 3
NCT02607930 Gilead Sciences HIV-1 Infection November 13, 2015 Phase 3
NCT02082808 ViiV Healthcare|GlaxoSmithKline Infection, Human Immunodeficiency Virus March 2014 Phase 1
NCT02351908 St Stephens Aids Trust|Merck Sharp & Dohme Corp. HIV March 2015 Phase 4
NCT02342769 ViiV Healthcare|GlaxoSmithKline Infection, Human Immunodeficiency Virus February 2015
NCT02028819 University of Colorado, Denver Human Immunodeficiency Virus (HIV) January 2012
NCT02519777 National Institute of Allergy and Infectious Diseases (NIAID) HIV Infections March 2016 Phase 4
NCT02868580 Neuroscience Trials Australia|Macquarie University, Australia|Westmead Hosptial|Calvary Health Care Bethlehem|The University of Sydney - Brain and Mind Centre Amyotrophic Lateral Sclerosis October 2016 Phase 1|Phase 2
NCT02386098 ViiV Healthcare|GlaxoSmithKline Infection, Human Immunodeficiency Virus July 8, 2015 Phase 2
NCT03110380 Gilead Sciences HIV-1-infection June 2017 Phase 3
NCT00796263 South East Asia Research Collaboration with Hawaii|Thai Red Cross AIDS Research Centre|Pfizer|Gilead Sciences|Merck Sharp & Dohme Corp.|ViiV Healthcare Acute HIV Infection April 2009 Phase 3
NCT03067285 Fundacion SEIMC-GESIDA HIV Infections July 1, 2017 Phase 4
NCT02259127 PENTA Foundation HIV Infection May 2016 Phase 2|Phase 3
NCT02961829 Federal University of São Paulo|Fundação de Amparo à Pesquisa do Estado de São Paulo|Conselho Nacional de Desenvolvimento Científico e Tecnológico|ViiV Healthcare Chronic Infection|HIV July 2015
NCT02583048 National Institute of Allergy and Infectious Diseases (NIAID) Tuberculosis|HIV Infections August 2016 Phase 2
NCT02938520 ViiV Healthcare|Janssen Pharmaceuticals|GlaxoSmithKline Infection, Human Immunodeficiency Virus October 27, 2016 Phase 3
NCT02569346 Radboud University HIV March 2016 Phase 1
NCT02075593 ViiV Healthcare|GlaxoSmithKline Infection, Human Immunodeficiency Virus January 1, 2015 Phase 3
NCT02588820 David Garcia Cinca|Fundacion Clinic per a la Recerca Biomédica|Hospital Clinic of Barcelona HIV Infections April 2016 Phase 3
NCT00042289 National Institute of Allergy and Infectious Diseases (NIAID)|Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD) HIV Infections March 2003 Phase 4
NCT00537966 University of Zurich HIV Infections January 2002
NCT02800655 mHealth UCSD|National Institute of Mental Health (NIMH)|Gilead Sciences|ViiV Healthcare|GlaxoSmithKline|Proteus Digital Health, Inc. HIV June 2016 Phase 4
NCT02858401 Gilead Sciences HIV-1 Infection January 29, 2015 Phase 1
NCT02285114 Gilead Sciences HIV-1 January 2015 Phase 2|Phase 3
NCT02302547 University Hospital, Tours|HOSPITAL, ORLEANS|Poitiers University Hospital|Centre Hospitalier de La Rochelle|HOSPITAL, SAINTES|HOSPITAL, FOCH|HOSPITAL, CAEN|HOSPITAL, HENRI MONDOR|HOSPITAL, HOTEL DIEU|HOSPITAL, CHARTRES|HOSPITAL, SAINT LOUIS|Tourcoing Hospital|HOSPITAL, NIORT|Tenon Hospital, Paris|Central Hospital, Nancy, France|University Hospital, Rouen HIV December 2014 Phase 3
NCT02605954 Gilead Sciences HIV-1 Infection November 18, 2015 Phase 3
NCT02354053 McGill University Health Center|ViiV Healthcare|CIHR Canadian HIV Trials Network HIV Infections November 2015 Phase 4
NCT02016924 Gilead Sciences Acquired Immune Deficiency Syndrome (AIDS)|HIV Infections January 16, 2014 Phase 2|Phase 3
NCT03160105 Calmy Alexandra|University Hospital, Geneva HIV-1-infection|Antiretroviral Therapy|Maintenance Therapy May 2017 Phase 4
NCT01939197 AbbVie Hepatitis C Virus Infection|Human Immunodeficiency Virus Infection|Chronic Hepatitis C|Compensated Cirrhosis and Non-cirrhotics August 2013 Phase 3
NCT02121795 Gilead Sciences HIV-1 Infection May 8, 2014 Phase 3
NCT02469246 Gilead Sciences HIV-1 Infection June 29, 2015 Phase 3
NCT02556268 Bayer HIV-DDI February 2016 Phase 1
NCT02616783 Gilead Sciences HIV-1 Infection December 22, 2015 Phase 3
NCT02449733 Emory University HIV May 2015
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References
Preparing Stock Solutions
Concentration Volume (DMSO) 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
Cell Assay
[1]

Dolutegravir (S/GSK1349572) is dissolved in stock solutions, and then diluted with appropriate media before use[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].

Animal Administration
[2]

Dolutegravir (S/GSK1349572) is formulated as a solution in N,N-dimethylacetamide and diluted with 50 mM N-methylglucamine in 3% mannitol (intravenous)[2].
Dolutegravir (S/GSK1349572) is formulated as a solution in D:Solutol:50 mM N-methylglucamine in 3% mannitol (1:1:8, v:w:v) (orally administered to fasted rats and monkeys)[2].
Dolutegravir (S/GSK1349572) is formulated as a suspension in 0.5% hydroxypropyl methylcellulose (HPMC)/0.1% polyoxyethylene sorbitan monooleate (Tween 80) (orally administered to non-fasted rats and monkeys)[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.

References
M.Wt

419.38

Formula

C₂₀H₁₉F₂N₃O₅

CAS No.

1051375-16-6

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: 10 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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