Name: Ertugliflozin L-pyroglutamic acid
Brand: Selleck Chemicals
SKU: S4431
Rating: 5 (1 reviews)

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

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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Signaling Pathway

SGLT Signaling Pathway

Choose Selective SGLT Inhibitors

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
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-01-11)
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

References

[1] Meiyan Jiang, Peter S Steyger. Expert Opin Ther Pat. 2015;25(11):1349-52.

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	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years -20°C powder		1 month-20°Cin solvent

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

Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.

In vivo Formulation Calculator

Preparing Stock Solutions

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Dilution Calculator Molecular Weight Calculator

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

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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