Ertugliflozin L-pyroglutamic acid Bioactivity,Chemical Properties,Storage & Solubility Information Pathways-PeptideDB

Description	Ertugliflozin L-pyroglutamic acid (PF-04971729 L-pyroglutamic acid) is a selective and orally active hSGLT2 inhibitor with an IC50 of 0.877 nM. Ertugliflozin L-pyroglutamic acid can be used for studies about the treatment of type 2 diabetes mellitus.
In vitro	Ertugliflozin L-pyroglutamic acid 展现出对SGLT2而非SGLT[2]的选择性高出2000倍以上。
In vivo	口服Ertugliflozin L-pyroglutamic 给大鼠所示出的结果为浓度依赖性的糖尿[2]。
Target activity	SGLT2 (human):0.877 nM
Synonyms	埃格列净, PF-04971729 L-pyroglutamic acid
molecular weight	566
Molecular formula	C27H32ClNO10
CAS	1210344-83-4
Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
Solubility	DMSO: 125 mg/mL (220.85 mM)
References	1. Miao Z, et al. Pharmacokinetics, metabolism, and excretion of the antidiabetic agent ertugliflozin (PF-04971729) in healthy male subjects. Drug Metab Dispos. 2013 Feb;41(2):445-56. 2. Kalgutkar AS, et al. Preclinical species and human disposition of PF-04971729, a selective inhibitor of the sodium-dependent glucose cotransporter 2 and clinical candidate for the treatment of type 2 diabetes mellitus. Drug Metab Dispos. 2011 Sep;39(9):1609-19. 3. Mascitti V, et al. Discovery of a clinical candidate from the structurally unique dioxa-bicyclo[3.2.1]octane class of sodium-dependent glucose cotransporter 2 inhibitors. J Med Chem. 2011 Apr 28;54(8):2952-60.

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