Ertugliflozin

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

For research use only.

Ertugliflozin (MK-8835, PF-04971729) 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.

Ertugliflozin Chemical Structure

CAS No. 1210344-57-2

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Biological Activity

Description Ertugliflozin (MK-8835, PF-04971729) 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 (from reference)

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 436.88
Formula

C22H25ClO7

CAS No. 1210344-57-2
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CCOC1=CC=C(C=C1)CC2=C(C=CC(=C2)C34C(C(C(C(O3)(CO4)CO)O)O)O)Cl

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04490681 Not yet recruiting Drug: Ertugliflozin|Drug: Placebo Heart Failure With Nonischemic Cardiomyopathy Yonsei University August 2020 Phase 3
NCT02115347 Completed Drug: Ertugliflozin 15 mg Type 2 Diabetes Mellitus|Hepatic Impairment Merck Sharp & Dohme LLC|Pfizer September 19 2014 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-08-01)

Tech Support

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.

Handling Instructions

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