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 No. 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

Ertugliflozin L-pyroglutamic acid Related Products

Signaling Pathway

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 Information & 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
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

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.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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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