Ertugliflozin L-pyroglutamic acid

Synonyms: MK-8835 L-pyroglutamic acid, PF-04971729 L-pyroglutamic acid

Ertugliflozin (MK-8835, PF-04971729) L-pyroglutamic acid is a potent, selective and orally active inhibitor of the sodium-dependent glucose cotransporter 2 (SGLT2) with IC50 of 0.877 nM for h-SGLT2. Ertugliflozin has the potential for the treatment of type 2 diabetes mellitus.

Ertugliflozin L-pyroglutamic acid Chemical Structure

Ertugliflozin L-pyroglutamic acid Chemical Structure

CAS: 1210344-83-4

Purity & Quality Control

Batch: S443101 DMSO] 100 mg/mL] false] Ethanol] 100 mg/mL] false] Water] 10 mg/mL] false Purity: 99.85%
99.85

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Biological Activity

Description Ertugliflozin (MK-8835, PF-04971729) L-pyroglutamic acid is a potent, selective and orally active inhibitor of the sodium-dependent glucose cotransporter 2 (SGLT2) with IC50 of 0.877 nM for h-SGLT2. Ertugliflozin has the potential for the treatment of type 2 diabetes mellitus.
Targets
h-SGLT2 [1]
(Cell-free assay)
0.877 nM
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 566 Formula

C27H32ClNO10

CAS No. 1210344-83-4 SDF --
Smiles CCOC1=CC=C(CC2=C(Cl)C=CC(=C2)C34OCC(CO)(O3)C(O)C(O)C4O)C=C1.OC(=O)C5CCC(=O)N5
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (176.67 mM); Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 100 mg/mL

Water : 10 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.

Handling Instructions

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