Home GPCR & G Protein SGLT inhibitor Ertugliflozin For research use only.

Ertugliflozin

Synonyms: MK-8835, PF-04971729

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

Ertugliflozin Chemical Structure

CAS: 1210344-57-2

Purity & Quality Control

Batch: S541301 DMSO] 87 mg/mL] false] Ethanol] 87 mg/mL] false] Water] 10.8 mg/mL] false Purity: 99.94%
99.94

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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
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
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].
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05727579 Not yet recruiting Diabetes Mellitus|Diabetic Kidney Disease|Hypertension Amsterdam UMC location VUmc|Merck Sharp & Dohme LLC|University of Colorado Denver June 1 2023 Phase 4
NCT04490681 Unknown status Heart Failure With Nonischemic Cardiomyopathy Yonsei University August 2020 Phase 3
NCT02115347 Completed Type 2 Diabetes Mellitus|Hepatic Impairment Merck Sharp & Dohme LLC|Pfizer September 19 2014 Phase 1

Chemical lnformation & Solubility

Molecular Weight 436.88 Formula

C22H25ClO7
CAS No. 1210344-57-2 SDF --
Smiles CCOC1=CC=C(C=C1)CC2=C(C=CC(=C2)C34C(C(C(C(O3)(CO4)CO)O)O)O)Cl
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 87 mg/mL ( (199.13 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 87 mg/mL

Water : 10.8 mg/mL


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

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

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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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.

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