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

Ertugliflozin Related Products

Signaling Pathway

Choose Selective SGLT Inhibitors

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 Information & 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


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo Formulation Calculator (Clear solution)

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

mg/kg g μL

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

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy Ertugliflozin | Ertugliflozin supplier | purchase Ertugliflozin | Ertugliflozin cost | Ertugliflozin manufacturer | order Ertugliflozin | Ertugliflozin distributor