[CAS NO. 1210344-57-2] Ertugliflozin

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PRODUCTS SPECIFICATIONS [1210344-57-2]

Catalog

HY-15461

Brand

MCE

CAS

1210344-57-2

DESCRIPTION [1210344-57-2]

Overview

MDL	MFCD21609259
Molecular Weight	436.88
Molecular Formula	C22H25ClO7
SMILES	ClC1=CC=C([C@]23O[C@@](CO)(CO3)[C@@H](O)[C@H](O)[C@H]2O)C=C1CC4=CC=C(OCC)C=C4

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

1 Publications Citing Use of MCE

[1]Biochem Pharmacol. 2016 Feb 1;101:27-39.

Summary

Ertugliflozin (PF-04971729) is a potent, selective and orally active inhibitor of the sodium-dependent glucose cotransporter 2 (SGLT2), with an IC ₅₀ of 0.877 nM for h-SGLT2 ^[1] . Has the potential for the treatment of type 2 diabetes mellitus ^[2] .

IC50 & Target

IC50: 0.877 nM (h-SGLT2) ^[1] .

In Vitro

Ertugliflozin (PF-04971729) demonstrates >2000-fold selectivity for SGLT2 inhibition (relative to SGLT1) in vitro ^[3] .

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

In Vivo

Ertugliflozin (PF-04971729) reveals a concentration-dependent glucosuria after oral administration to rats ^[3] .

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

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT01018823	Merck Sharp & Dohme LLC\|Pfizer	Healthy Volunteer	December 14, 2009	Phase 1
NCT02099110	Merck Sharp & Dohme LLC\|Pfizer	Type 2 Diabetes Mellitus	April 22, 2014	Phase 3
NCT03640221	Cedars-Sinai Medical Center\|Merck Sharp & Dohme LLC	Hypertension\|Diabetes Mellitus, Type 2	September 1, 2018	Phase 4
NCT02033889	Merck Sharp & Dohme LLC\|Pfizer	Type 2 Diabetes Mellitus	December 13, 2013	Phase 3
NCT04231331	Asan Medical Center\|Merck Sharp & Dohme LLC	Mitral Valve Insufficiency\|Left Ventricular Systolic Dysfunction	November 4, 2020	Phase 3
NCT04027530	Amsterdam UMC, location VUmc	Type 2 Diabetes Mellitus\|Diabetic Kidney Disease\|Diabetic Nephropathy\|Renal Hypoxia\|Renoprotection\|SGLT2 Inhibitor\|Ertugliflozin	December 10, 2020	Phase 4
NCT05152940	Icahn School of Medicine at Mount Sinai	Heart Failure With Reduced Ejection Fraction\|Congestion	November 2022	Phase 4
NCT04438213	Yale University\|Merck Sharp & Dohme LLC	Heart Failure	March 10, 2021	Phase 2
NCT05612594	Yale University\|Case Western Reserve University	Sleep Apnea	November 2022	Phase 4
NCT01114568	Merck Sharp & Dohme LLC\|Pfizer	Healthy	May 2010	Phase 1
NCT04167761	Stanford University\|Merck Sharp & Dohme LLC	Cardiovascular Diseases\|Atherosclerosis\|Type 2 Diabetes\|Insulin Resistance	July 1, 2020	Early Phase 1
NCT04029480	Merck Sharp & Dohme LLC\|Pfizer	Type 2 Diabetes Mellitus	October 8, 2019	Phase 3
NCT02226003	Merck Sharp & Dohme LLC\|Pfizer	Type 2 Diabetes Mellitus	September 23, 2014	Phase 3
NCT01986881	Merck Sharp & Dohme LLC\|Pfizer	Type 2 Diabetes Mellitus	November 4, 2013	Phase 3
NCT01223339	Merck Sharp & Dohme LLC\|Pfizer	Diabetes Mellitus, Type 2	October 2010	Phase 1
NCT04490681	Yonsei University	Heart Failure With Nonischemic Cardiomyopathy	August 2020	Phase 3
NCT02115347	Merck Sharp & Dohme LLC\|Pfizer	Type 2 Diabetes Mellitus\|Hepatic Impairment	September 19, 2014	Phase 1
NCT01986855	Merck Sharp & Dohme LLC\|Pfizer	Type 2 Diabetes Mellitus	December 2, 2013	Phase 3
NCT01096667	Merck Sharp & Dohme LLC\|Pfizer	Diabetes Mellitus, Type 2\|Hypertension	May 17, 2010	Phase 2
NCT03717194	Soo Lim\|MSD Korea Ltd.\|Seoul National University Bundang Hospital	Type2 Diabetes\|Heart Failure	June 1, 2019	Phase 3
NCT00989079	Merck Sharp & Dohme LLC\|Pfizer	Type 2 Diabetes Mellitus	October 16, 2009	Phase 1
NCT02630706	Merck Sharp & Dohme LLC\|Pfizer	Type 2 Diabetes Mellitus	December 16, 2015	Phase 3
NCT01059825	Merck Sharp & Dohme LLC\|Pfizer	Diabetes Mellitus, Type 2	February 24, 2010	Phase 2
NCT03416270	University Health Network, Toronto\|University Medical Center Groningen\|Merck Sharp & Dohme LLC\|University of Toronto\|Toronto General Hospital	Type 2 Diabetes Mellitus\|Heart Failure	May 7, 2018	Phase 2
NCT01127308	Merck Sharp & Dohme LLC\|Pfizer	Type 2 Diabetes Mellitus (T2DM)	June 2010	Phase 1
NCT02036515	Merck Sharp & Dohme LLC\|Pfizer	Type 2 Diabetes Mellitus	March 12, 2014	Phase 3
NCT01054300	Merck Sharp & Dohme LLC\|Pfizer	Diabetes Mellitus, Type 2\|Adult	February 17, 2010	Phase 1
NCT01958671	Merck Sharp & Dohme LLC\|Pfizer	Type 2 Diabetes Mellitus	October 9, 2013	Phase 3
NCT01948986	Merck Sharp & Dohme LLC\|Pfizer	Renal Impairment\|Type 2 Diabetes Mellitus	October 1, 2013	Phase 1
NCT02411929	Merck Sharp & Dohme LLC\|Pfizer	Type 2 Diabetes Mellitus	October 29, 2014	Phase 1
NCT01999218	Merck Sharp & Dohme LLC\|Pfizer	Type 2 Diabetes Mellitus	December 16, 2013	Phase 3
NCT04600921	Medical University of Graz\|Klinikum Klagenfurt am Wörthersee\|Elisabethinen Hospital\|Klinik Ottakring\|Medical University Innsbruck\|Medical University of Vienna\|General Hospital Linz\|Landesklinkum Wiener Neustadt	Heart Failure With Reduced Ejection Fraction\|Heart Failure With Mid Range Ejection Fraction\|Implantable Cardioverter-Defibrillators\|Cardiac Resynchronization Therapy	June 24, 2021	Phase 3
NCT04071626	University Hospitals Cleveland Medical Center	Heart Failure, Diastolic\|Diabetes Mellitus, Type 2	March 1, 2020	Phase 4

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 : 250 mg/mL ( 572.24 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.2890 mL	11.4448 mL	22.8896 mL
5 mM	0.4578 mL	2.2890 mL	4.5779 mL
10 mM	0.2289 mL	1.1445 mL	2.2890 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: ≥ 2.08 mg/mL (4.76 mM); Clear solution
2.

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

Solubility: ≥ 2.08 mg/mL (4.76 mM); Clear solution
3.

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

Solubility: ≥ 2.08 mg/mL (4.76 mM); Clear solution

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

References

Synonyms

β-L-Idopyranose, 1,6-anhydro-1-C-[4-chloro-3-[(4-ethoxyphenyl)methyl]phenyl]-5-C-(hydroxymethyl)-

1,6-Anhydro-1-C-[4-chloro-3-[(4-ethoxyphenyl)methyl]phenyl]-5-C-(hydroxymethyl)-β-L-idopyranose

Ertugliflozin

PF 04971729-00

PF 04971729

MK 8835