Ertugliflozin

Catalog No.S5413 Synonyms: MK-8835, PF-04971729

Ertugliflozin Chemical Structure

Molecular Weight(MW): 436.88

Ertugliflozin is a potent and selective sodium-dependent glucose cotransporter 2 inhibitor with IC50 values of 0.877 nM for h-SGLT2 and 1000-fold higher for h-SGLT1.

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Biological Activity

Description Ertugliflozin is a potent and selective sodium-dependent glucose cotransporter 2 inhibitor with IC50 values of 0.877 nM for h-SGLT2 and 1000-fold higher for h-SGLT1.
Targets
hSGLT2 [1]
(Cell-free assay)
0.877 nM
In vitro

Ertugliflozin (it is claimed) has a 2000-fold increase in selectivity for human SGLT2 over SGLT1 (IC50: SGLT2 = 0.877 nM vs SGLT1 = 1960 nM) in vitro[1].

In vivo Ertugliflozin is rapidly absorbed in preclinical species after oral administration, and it is characterized by low clearance (excreted in the urine in preclinical species) and a moderate steady-state distribution volume. There is low potential for pharmacokinetic interaction of ertugliflozin. Ertugliflozin is well absorbed in humans and eliminated largely via glucuronidation. Ertugliflozin improved glycemic control, body weight and blood pressure in patients with T2DM suboptimally controlled by metformin, and is well-tolerated[1].

Protocol

Solubility (25°C)

In vitro DMSO 87 mg/mL (199.13 mM)
Water 87 mg/mL (199.13 mM)
Ethanol 87 mg/mL (199.13 mM)

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 436.88
Formula

C22H25ClO7

CAS No. 1210344-57-2
Storage powder
in solvent
Synonyms MK-8835, PF-04971729

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03717194 Recruiting Type2 Diabetes|Heart Failure Soo Lim|MSD Korea Ltd.|Seoul National University Bundang Hospital April 1 2019 Phase 3
NCT03717194 Recruiting Type2 Diabetes|Heart Failure Soo Lim|MSD Korea Ltd.|Seoul National University Bundang Hospital April 1 2019 Phase 3
NCT03640221 Not yet recruiting Hypertension|Diabetes Mellitus Type 2 Cedars-Sinai Medical Center|Merck Sharp & Dohme Corp. September 1 2018 Phase 4
NCT03640221 Not yet recruiting Hypertension|Diabetes Mellitus Type 2 Cedars-Sinai Medical Center|Merck Sharp & Dohme Corp. September 1 2018 Phase 4
NCT03416270 Not yet recruiting Type 2 Diabetes Mellitus|Heart Failure University Health Network Toronto|University Medical Center Groningen|Merck Sharp & Dohme Corp.|University of Toronto|Toronto General Hospital May 7 2018 Phase 2
NCT03416270 Not yet recruiting Type 2 Diabetes Mellitus|Heart Failure University Health Network Toronto|University Medical Center Groningen|Merck Sharp & Dohme Corp.|University of Toronto|Toronto General Hospital May 7 2018 Phase 2

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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SGLT Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID