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[CAS NO. 928672-86-0] Canagliflozin hemihydrate

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Catalog:	HY-I0383
Brand:	MCE
CAS:	928672-86-0

Overview

MDL	MFCD28975933
Molecular Weight	453.52
Molecular Formula	C24H26FO5.5S
SMILES	CC1=CC=C([C@H]2[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O2)C=C1CC3=CC=C(C4=CC=C(F)C=C4)S3.[0.5H2O]

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

18 Publications Citing Use of MCE

[1]Nature. 2018 Aug;560(7719):499-503.
[2]Nat Cell Biol. 2022 May 30.
[3]Mol Cell. 2020 Oct 1;80(1):87-101.e5.
[4]Cardiovasc Res. 02 November 2020.
[5]Mol Metab. 2019 Jan;19:1-12.
[6]Biochem Pharmacol. 2020 May;175:113856.
[7]Biochem Pharmacol. 2018 Jun;152:45-59.
[8]J Am Heart Assoc. 2022 Jul 29;e025328.
[9]Biomed Pharmacother. 2023 Jan 7;159:114228.
[10]Biomed Pharmacother. 2020 Dec;132:110821.
[11]Vascul Pharmacol. 2018 Oct;109:56-71.
[12]Sci Rep. 2021 Jul 1;11(1):13700.
[13]Int Immunopharmacol. 2020 Nov;88:106969.
[14]Int J Oncol. 2020 Nov;57(5):1223-1233.
[15]Int J Med Sci. 2018 Jun 13;15(9):937-943.
[16]Mol Med Rep. 2021 Oct;24(4):703.
[17]Biomed Chromatogr. 2019 Nov;33(11):e4663.
[18]Biomed Chromatogr. 2016 Oct;30(10):1549-55.

Summary

Canagliflozin hemihydrate (JNJ28431754 hemihydrate) is a selective SGLT2 inhibitor with IC ₅₀ s of 2 nM, 3.7 nM, and 4.4 nM for mSGLT2, rSGLT2, and hSGLT2 in CHOK cells, respectively ^[1] .

IC50 & Target

IC50: 2/3.7/4.4 nM (mSGLT2/rSGLT2/hSGLT2, in CHOK cells) ^[1]

In Vitro

Canagliflozin inhibits Na ⁺ -dependent ¹⁴ C-AMG uptake in CHO-hSGLT2 cells, with an IC ₅₀ of 4.4±1.2 nM. Similar IC ₅₀ values are obtained in CHO-rSGLT2 and CHO-mSGLT2 cells (IC ₅₀ = 3.7 and 2.0 nM for rat and mouse SGLT2, respectively). Canagliflozin inhibits ¹⁴ C-AMG uptake in CHO-hSGLT1 and mSGLT1 cells with IC ₅₀ of 684±159 nM and >1,000 nM, respectively ^[1] .

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

In Vivo

Canagliflozin (30 mg/kg treatment for 4 weeks) reduced blood glucose (BG) levels, respiratory exchange ratio, and body weight gain in DIO mice ^[1] .
Canagliflozin (3 mg/kg for 3 weeks) increases urinary glucose excretion (UGE) with no significant change in total food intake compared with that in vehicle-treated rats, leading to a decrease in body weight In ZF rats ^[1] .

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

Animal Model:	Diet-induced obese, insulin resistantmice (DIO) Mice ^[1]
Dosage:	30 mg/kg
Administration:	Oral gavage; daily; 4 weeks
Result:	Reduced BG levels, respiratory exchange ratio, and body weight gain.

Animal Model:	Male Zucker fatty (ZF) obese, insulin resistant rats ^[1]
Dosage:	3 mg/kg
Administration:	Oral gavage; daily; 3 weeks
Result:	UGE was increased with no significant change in total food intake compared with that in vehicle-treated rats, leading to a decrease in body weight.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT02846506	Janssen Research & Development, LLC	Healthy	August 2016	Phase 1
NCT03492580	Janssen Research & Development, LLC	Diabetes Mellitus, Type 2\|Cardiovascular Diseases	February 22, 2018
NCT05090358	Memorial Sloan Kettering Cancer Center	Breast Cancer\|Breast Cancer Stage IV\|Metastatic Breast Cancer	October 8, 2021	Phase 2
NCT01508182	Janssen Research & Development, LLC	Healthy	January 2012	Phase 1
NCT02462421	University of Maryland, Baltimore\|National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK)	Diabetes Mellitus\|Gout\|Hyperuricemia	June 1, 2015	Phase 4
NCT02653209	Royal Devon and Exeter NHS Foundation Trust\|University of Exeter\|NHS Tayside\|University of Dundee\|University of Glasgow\|Newcastle University\|King´s College London	Type 2 Diabetes	November 1, 2016	Phase 4
NCT02912455	The Cleveland Clinic\|Janssen Scientific Affairs, LLC	Diabetes Mellitus, Type 2\|Obesity	January 5, 2017	Phase 4
NCT04796428	Center for Outcomes Research and Clinical Epidemiology, Italy\|Italian Society of Diabetology	Diabetes Mellitus, Type 2	June 30, 2021	Phase 4
NCT02673138	Yale University\|National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK)	Type 1 Diabetes	January 2016	Not Applicable
NCT03267576	Janssen Research & Development, LLC	Diabetes Mellitus, Type 2	October 27, 2017	Phase 4
NCT02227849	Mitsubishi Tanabe Pharma Corporation	Type 2 Diabetes Mellitus	August 2014	Phase 4
NCT01273558	Johnson & Johnson Pharmaceutical Research & Development, L.L.C.	Diabetes Mellitus, Type 2	January 2011	Phase 1
NCT04073680	Petra Pharma	Breast Cancer\|Endometrial Cancer\|Lung Cancer\|Colo-rectal Cancer\|Head and Neck Cancer	September 1, 2020	Phase 1\|Phase 2
NCT02891954	University of Maryland, Baltimore\|National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK)	Diabetes Mellitus, Type 2	September 2016	Phase 1
NCT05507892	University of Colorado, Denver\|Boston Medical Center\|University of Michigan\|Brigham and Women´s Hospital	Type 2 Diabetes\|Diabetic Kidney Disease	October 10, 2022	Phase 2
NCT02624908	Foundation for Atlanta Veterans Education and Research, Inc.\|Janssen Scientific Affairs, LLC	Diabetes Mellitus, Type 2	January 2016	Phase 4
NCT01081834	Janssen Research & Development, LLC	Diabetes Mellitus, Type 2	March 2010	Phase 3
NCT01395927	Johnson & Johnson Pharmaceutical Research & Development, L.L.C.	Healthy	July 2011	Phase 1
NCT01064414	Janssen Research & Development, LLC	Diabetes Mellitus, Type 2\|Renal Insufficiency	June 2010	Phase 3
NCT01128985	Johnson & Johnson Pharmaceutical Research & Development, L.L.C.	Diabetes Mellitus, Type 2	March 2010	Phase 1
NCT01665638	Janssen-Cilag International NV	Healthy	September 2012	Phase 1
NCT03136484	Novo Nordisk A+S	Diabetes\|Diabetes Mellitus, Type 2	March 15, 2017	Phase 3
NCT02622113	Mitsubishi Tanabe Pharma Corporation	Type 2 Diabetes Mellitus	December 2014	Phase 4
NCT02065791	Janssen Research & Development, LLC\|The George Institute for Global Health, Australia	Diabetes Mellitus, Type 2\|Diabetic Nephropathy	February 17, 2014	Phase 3
NCT02851095	Janssen Research & Development, LLC	Healthy	August 2016	Phase 1
NCT01809327	Janssen Research & Development, LLC	Diabetes Mellitus, Type 2	June 4, 2013	Phase 3
NCT01157000	Johnson & Johnson Pharmaceutical Research & Development, L.L.C.	Healthy	May 2010	Phase 1
NCT03436693	Mitsubishi Tanabe Pharma Corporation	Diabetic Nephropathy	February 15, 2018	Phase 3
NCT01508195	Janssen Research & Development, LLC	Healthy	January 2012	Phase 1
NCT05364190	October 6 University\|Cairo University\|National Heart Institute, Egypt	Chronic Heart Failure\|Acute Decompensated Heart Failure\|Diabetes Mellitus	June 4, 2022	Phase 3
NCT03170518	Janssen Research & Development, LLC	Diabetes Mellitus, Type 2	July 21, 2017	Phase 3
NCT02139943	Janssen Research & Development, LLC	Diabetes Mellitus, Type 1	May 2014	Phase 2
NCT01756404	Johnson & Johnson Pharmaceutical Research & Development, L.L.C.	Healthy	June 14, 2007	Phase 1
NCT01877889	Janssen-Cilag International NV	Healthy	July 2013	Phase 1
NCT02865668	Janssen Research & Development, LLC	Healthy	August 2016	Phase 1
NCT02324842	The University of Texas Health Science Center at San Antonio\|Janssen Scientific Affairs, LLC	Type 2 Diabetes Mellitus	November 2014	Not Applicable
NCT03249506	Janssen Research & Development, LLC	Diabetes Mellitus, Type 2	May 12, 2016
NCT03604224	Johnson & Johnson Private Limited	Diabetes Mellitus, Type 2	September 5, 2018
NCT00642278	Johnson & Johnson Pharmaceutical Research & Development, L.L.C.	Diabetes Mellitus, Type II\|Diabetes Mellitus, Non Insulin Dependent	April 2008	Phase 2
NCT01137812	Janssen Research & Development, LLC	Diabetes Mellitus, Type 2	July 2010	Phase 3
NCT05367063	Shanghai Zhongshan Hospital	Type 2 Diabetes\|Cardiovascular Diseases\|Cardiac Perfusion Defect	January 5, 2022	Phase 4
NCT01186588	Johnson & Johnson Pharmaceutical Research & Development, L.L.C.	Healthy\|Hepatic Insufficiency	August 2010	Phase 1
NCT04252287	Janssen Research & Development, LLC	Heart Failure	March 10, 2020	Phase 3
NCT05135039	xiaolong zhao\|Huashan Hospital	PreDiabetes\|Hiv	January 1, 2022	Not Applicable
NCT04288778	Johnson & Johnson Private Limited	Diabetes Mellitus	November 25, 2020	Phase 4
NCT01483781	Janssen Research & Development, LLC	Diabetes Mellitus, Type 2\|Plasma Volume	December 2011	Phase 1
NCT00968812	Janssen Research & Development, LLC	Diabetes Mellitus, Type 2	September 2009	Phase 3
NCT01343290	Johnson & Johnson Pharmaceutical Research & Development, L.L.C.	Healthy	April 2011	Phase 1
NCT02360774	Beth Israel Deaconess Medical Center\|Janssen Scientific Affairs, LLC	Type 2 Diabetes\|Overweight\|Obesity	February 2015	Phase 4
NCT04973891	Shengjing Hospital	Polycystic Ovary Syndrome	April 7, 2021	Phase 1\|Phase 2
NCT01032629	Janssen Research & Development, LLC\|The George Institute for Global Health, Australia	Diabetes Mellitus, Type 2\|Cardiovascular Diseases\|Risk Factors	December 9, 2009	Phase 3
NCT01281579	Johnson & Johnson Pharmaceutical Research & Development, L.L.C.	Healthy	January 2011	Phase 1
NCT01106690	Janssen Research & Development, LLC	Diabetes Mellitus, Type 2	June 2010	Phase 3
NCT02220920	Mitsubishi Tanabe Pharma Corporation	Type 2 Diabetes Mellitus	August 2014	Phase 4
NCT02354235	Mitsubishi Tanabe Pharma Corporation	Type 2 Diabetes Mellitus	January 2015	Phase 3
NCT00963768	Johnson & Johnson Pharmaceutical Research & Development, L.L.C.	Diabetes Mellitus, Type 2	June 2007	Phase 1
NCT02920918	Virginia Commonwealth University\|Janssen Scientific Affairs, LLC	Heart Failure, Systolic\|Diabetes Mellitus, Type 2	October 2016	Phase 4
NCT02354222	Mitsubishi Tanabe Pharma Corporation	Type 2 Diabetes Mellitus	January 2015	Phase 3
NCT01286103	Johnson & Johnson Pharmaceutical Research & Development, L.L.C.	Healthy	January 2011	Phase 1
NCT02597309	Joslin Diabetes Center	Diabetes, Obesity	November 2015	Phase 4
NCT03190798	The University of Texas Health Science Center at San Antonio\|Janssen Scientific Affairs, LLC	Type2 Diabetes Mellitus\|Cardiovascular Diseases	September 1, 2017	Phase 4
NCT03426956	Hvidovre University Hospital	Overweight	February 8, 2018	Not Applicable
NCT01707316	Janssen Research & Development, LLC	Healthy	June 2012	Phase 1
NCT01733108	Johnson & Johnson Pharmaceutical Research & Development, L.L.C.	Healthy	July 2008	Phase 1
NCT02851212	Janssen Research & Development, LLC	Healthy	August 2016	Phase 1
NCT01939496	Janssen Scientific Affairs, LLC	Diabetes Mellitus, Type 2\|Hypertension	October 2013	Phase 4
NCT01381900	Janssen Research & Development, LLC	Diabetes Mellitus, Type 2	August 2011	Phase 3
NCT02142309	University of Campania Luigi Vanvitelli	Type 2 Diabetes	October 2005	Phase 4
NCT02221180	Janssen Research & Development, LLC	Bioequivalence	August 2014	Phase 1
NCT01718652	Johnson & Johnson Pharmaceutical Research & Development, L.L.C.	Healthy	February 2011	Phase 1
NCT01759576	Johnson & Johnson Pharmaceutical Research & Development, L.L.C.	Renal Insufficiency\|Healthy	March 2008	Phase 1
NCT02000700	Janssen Research & Development, LLC	Diabetes Mellitus, Type 2	March 2014	Phase 1
NCT02964585	George Washington University\|Janssen Scientific Affairs, LLC	Type 2 Diabetes Mellitus	November 2016	Phase 4
NCT01381887	Johnson & Johnson Pharmaceutical Research & Development, L.L.C.	Diabetes Mellitus, Type 2	June 2011	Phase 1
NCT01177163	Johnson & Johnson Pharmaceutical Research & Development, L.L.C.	Diabetes Mellitus, Type 2	May 2008	Phase 1
NCT01294631	Johnson & Johnson Pharmaceutical Research & Development, L.L.C.	Healthy	March 2011	Phase 1
NCT05347459	Alexandria University	Type 2 Diabetes	March 2, 2022
NCT01177150	Johnson & Johnson Pharmaceutical Research & Development, L.L.C.	Healthy	November 2006	Phase 1
NCT04014192	Peking Union Medical College Hospital	Type 2 Diabetes Mellitus	September 1, 2019	Phase 4
NCT00650806	Johnson & Johnson Pharmaceutical Research & Development, L.L.C.	Obesity	May 2008	Phase 2
NCT03298009	Université de Sherbrooke\|Janssen Inc.	Type2 Diabetes\|Heart Failure	November 1, 2017	Not Applicable
NCT01787357	Johnson & Johnson Pharmaceutical Research & Development, L.L.C.	Healthy	June 2008	Phase 1
NCT01714193	Johnson & Johnson Pharmaceutical Research & Development, L.L.C.	Healthy	February 2008	Phase 1
NCT02220218	Janssen Research & Development, LLC	Healthy	August 2014	Phase 1
NCT01748526	Johnson & Johnson Pharmaceutical Research & Development, L.L.C.	Healthy	August 2008	Phase 1
NCT02404870	National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK)\|National Institutes of Health Clinical Center (CC)	Healthy Volunteers	September 16, 2014	Phase 1
NCT01756417	Johnson & Johnson Pharmaceutical Research & Development, L.L.C.	Healthy	October 2007	Phase 1
NCT01106677	Janssen Research & Development, LLC	Diabetes Mellitus, Type 2	May 2010	Phase 3
NCT01714206	Johnson & Johnson Pharmaceutical Research & Development, L.L.C.	Healthy	June 2009	Phase 1
NCT01821027	Johnson & Johnson Pharmaceutical Research & Development, L.L.C.	Healthy	August 2008	Phase 1
NCT05422092	First Affiliated Hospital Xi´an Jiaotong University	Type 2 Diabetes Mellitus With Complication	September 20, 2022	Not Applicable
NCT05427084	Ottawa Heart Institute Research Corporation	Diabetes Type 2\|Coronary Artery Disease	September 2022	Phase 2\|Phase 3
NCT01340664	Janssen Research & Development, LLC	Diabetes Mellitus, Type 2	July 2011	Phase 2
NCT04720859	Hospital Universitari Vall d´Hebron Research Institute	Postprandial Hypoglycemia	January 5, 2018	Not Applicable
NCT01106625	Janssen Research & Development, LLC	Diabetes Mellitus, Type 2	May 2010	Phase 3
NCT01916863	Lexicon Pharmaceuticals	Healthy Subjects	August 2013	Phase 1
NCT01106651	Janssen Research & Development, LLC	Diabetes Mellitus, Type 2	June 2010	Phase 3
NCT05513729	First Affiliated Hospital Xi´an Jiaotong University	Type 2 Diabetes Mellitus With Complication	August 18, 2022
NCT03936010	Brigham and Women´s Hospital	Diabetes	September 22, 2017
NCT02694263	University of Leicester\|University Hospital Birmingham	Diabetes Mellitus, Type 2	July 2016	Phase 4
NCT02243202	Janssen Research & Development, LLC	Obesity	September 2014	Phase 2
NCT01463774	Janssen Research & Development, LLC	Healthy	September 2011	Phase 1

Appearance

Solid

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 : ≥ 100 mg/mL ( 220.50 mM )

* "≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.2050 mL	11.0249 mL	22.0497 mL
5 mM	0.4410 mL	2.2050 mL	4.4099 mL
10 mM	0.2205 mL	1.1025 mL	2.2050 mL

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

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.5 mg/mL (5.51 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (5.51 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.5 mg/mL (5.51 mM); Clear solution

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

References

[1] Liang Y, et al. Effect of canagliflozin on renal threshold for glucose, glycemia, and body weight in normal and diabetic animal models. PLoS One. 2012;7(2):e30555.

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