Ertugliflozin

For research use only.

Catalog No.S5413 Synonyms: MK-8835, PF-04971729

Ertugliflozin Chemical Structure

Molecular Weight(MW): 436.88

Ertugliflozin 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.

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Biological Activity

Description Ertugliflozin 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

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 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].

Protocol

Solubility (25°C)

In vitro DMSO 87 mg/mL (199.13 mM)
Water 87 mg/mL (199.13 mM)
Ethanol 87 mg/mL (199.13 mM)

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 436.88
Formula

C22H25ClO7

CAS No. 1210344-57-2
Storage powder
in solvent
Synonyms MK-8835, PF-04971729
Smiles CCOC1=CC=C(CC2=C(Cl)C=CC(=C2)C34OCC(CO)(O3)C(O)C(O)C4O)C=C1

In vivo Formulation Calculator (Clear solution)

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

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

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Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

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Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
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Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02115347 Completed Drug: Ertugliflozin 15 mg Type 2 Diabetes Mellitus|Hepatic Impairment Merck Sharp & Dohme Corp.|Pfizer September 19 2014 Phase 1
NCT01948986 Completed Drug: Ertugliflozin Renal Impairment|Type 2 Diabetes Mellitus Merck Sharp & Dohme Corp.|Pfizer October 1 2013 Phase 1
NCT01223339 Completed Drug: Ertugliflozin|Drug: Placebo Diabetes Mellitus Type 2 Merck Sharp & Dohme Corp.|Pfizer October 2010 Phase 1

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

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SGLT Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID