MK-8835, PF-04971729 Cas:1210344-57-2

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Product Description:

Product Name: MK-8835, PF-04971729 CAS NO: 1210344-57-2        

                                       

Synonyms:

(1S,2S,3S,4R,5S)-5-[4-chloro-3-[(4-ethoxyphenyl)methyl]phenyl]-1-(hydroxymethyl)-6,8-dioxabicyclo[3.2.1]octane-2,3,4-triol;

PF-04971729;

Ertugliflozin (USAN/INN);

 

Chemical & Physical Properties:

Appearance: A crystalline solid

Assay :≥99.0%

Density: 1.455 g/cm3

Boiling Point: 630.5±55.0℃(Predicted)

Vapor Pressure: 0.0±1.9 mmHg at 25℃

Index of Refraction: 1.652

 

Egla is a new class of SGLT2 inhibitors jointly developed by Pfizer and Merck. Steglatro was approved by FDA in December, 2011 for the treatment of adult patients with type 2 diabetes. It has not yet been marketed in China. Ertugliflozin (PF-04971729) is a potent, selective and orally active inhibitor of the sodium-dependent glucose cotransporter 2 (SGLT2), with an IC50 of 0.877 nM for h-SGLT2. A drug for the treatment of type 2 diabetes mellitus.

PF-04971729, a potent and selective inhibitor of the sodium-dependent glucose cotransporter 2, is currently in phase 2 trials for the treatment of diabetes mellitus. Inhibitory effects against the organic cation transporter 2-mediated uptake of [14C]metformin by PF-04971729 also were very weak (IC50 900μM).The disposition of PF-04971729, an orally active selective inhibitor of the sodium-dependent glucose cotransporter 2, was studied after a single 25-mg oral dose of [14C]-PF-04971729 to healthy human subjects. The absorption of PF-04971729 in humans was rapid with a Tmax at ~ 1.0 h. Of the total radioactivity excreted in feces and urine, unchanged PF-04971729 collectively accounted for ~ 35.3% of the dose, suggestive of moderate metabolic elimination in humans.

 

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