Ertugliflozin L-pyroglutamic acid

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CAS NO:

1210344-83-4

Ertugliflozin (PF-04971729) L-pyroglutamic acid 是有效的、选择性的、具有口服活性的钠离子依赖的葡萄糖协同转运蛋白2 (SGLT2) 的有效选择性抑制剂。其对h-SGLT2 的 IC50 值为0.877 nM。是一种治疗2型糖尿病的临床药物。

Cas No.	1210344-83-4
别名	埃格列净,PF-04971729 L-pyroglutamic acid
Canonical SMILES	ClC1=CC=C([C@]23O[C@@](CO)(CO3)[C@@H](O)[C@H](O)[C@H]2O)C=C1CC4=CC=C(OCC)C=C4.O=C5CC[C@@H](C(O)=O)N5
分子式	C₂₇H₃₂ClNO₁₀
分子量	566
溶解度	DMSO: ≥ 125 mg/mL (220.85 mM)
储存条件	Store at -20°C
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request
产品描述	Ertugliflozin (PF-04971729) L-pyroglutamic acid 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[1]. A drug for the treatment of type 2 diabetes mellitus[2]. IC50: 0.877 nM (h-SGLT2)[1]. Ertugliflozin (PF-04971729) demonstrates >2000-fold selectivity for SGLT2 inhibition (relative to SGLT1) in vitro[3]. Ertugliflozin (PF-04971729) reveals a concentration-dependent glucosuria after oral administration to rats[3]. [1]. 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. [2]. 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. [3]. 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.