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Ertugliflozin L-pyroglutamic acid SGLT inhibitor

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

Cat.No.S4431

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.

Chemical Structure

Molecular Weight: 566

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Quality Control

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

Cited in Nature Medicine for its top-tier quality
COA
SDS
Datasheet

99.85

Related Targets	Bcl-2 Caspase PD-1/PD-L1 Ferroptosis p53 Apoptosis related Synthetic Lethality STAT TNF-alpha Ras
Other SGLT Inhibitors	Sotagliflozin (LX4211) Phlorizin Phloretin (RJC 02792) Tofogliflozin(CSG 452) Ipragliflozin L-Proline Ipragliflozin (ASP1941) Swertisin KGA-2727 Mizagliflozin (KWA 0711) Bexagliflozin (EGT1442)

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (176.67 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 100 mg/mL

Water : 10 mg/mL

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

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.

Chemical Information, Storage & Stability

Molecular Weight	566	Formula	C₂₇H₃₂ClNO₁₀	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	1210344-83-4	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	MK-8835 L-pyroglutamic acid, PF-04971729 L-pyroglutamic acid			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

Mechanism of Action

Targets/IC₅₀/Ki	h-SGLT2 (Cell-free assay) 0.877 nM
References	[1] https://pubmed.ncbi.nlm.nih.gov/26291462/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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Handling Instructions

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