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[CAS NO. 1210344-57-2] Ertugliflozin
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-15461 |
| Brand: | MCE |
| CAS: | 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 |
1 Publications Citing Use of MCE
Summary
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
DMSO : 250 mg/mL ( 572.24 mM ; Need ultrasonic)
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 |
References
- [1] Mascitti V, et al. Discovery of a clinical candidate from the structurally unique dioxa-bicyclo[3.2.1]octane class of sodium-dependent glucose cotransporter 2 inhibitors. J Med Chem. 2011 Apr 28;54(8):2952-60.
- [2] Miao Z, et al. Pharmacokinetics, metabolism, and excretion of the antidiabetic agent ertugliflozin (PF-04971729) in healthy male subjects. Drug Metab Dispos. 2013 Feb;41(2):445-56.
- [3] Kalgutkar AS, et al. Preclinical species and human disposition of PF-04971729, a selective inhibitor of the sodium-dependent glucose cotransporter 2 and clinical candidate for the treatment of type 2 diabetes mellitus. Drug Metab Dispos. 2011 Sep;39(9):16
Synonyms
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