Ertugliflozin-L-pyroglutamic-acid-PF-04971729-L-pyroglutamic-acid-DataSheet-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEErtugliflozin L-pyroglutamic acidCat. No.: HY-15461ACAS No.: 1210344-83-4Synonyms: PF-04971729 L-pyroglutamic acid分式: CHClNO分量: 566作靶点: SGLT作通路: Membrane Transporter/Ion Channel储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6

2、 months-20C 1 month溶解性数据体外实验 DMSO : 125 mg/mL (220.85 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 1.7668 mL 8.8339 mL 17.6678 mL5 mM 0.3534 mL 1.7668 mL 3.5336 mL10 mM 0.1767 mL 0.8834 mL 1.7668 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。体内实验请根据您的

3、实验动物和给药式选择适当的溶解案，配制前请先配制澄清的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄清的储备液可以根据储存条件，适当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (3.67 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.08 mg/mL (3.67

4、mM); Clear solution1/2 Master of Small Molecules 您边的抑制剂师www.MedChemE3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.08 mg/mL (3.67 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Ertugliflozin (PF-04971729) L-pyroglutamic acid有效的、选择性的、具有服活性的钠离依赖的葡萄糖协同转运蛋2 (SGLT2) 的有效选择性抑制剂。其对h-SGLT2 的 IC50 值为0.877 nM 1 2

5、。 种治疗2型糖尿病的临床药物 3。IC50 & Target IC50: 0.877 nM (h-SGLT2) 1.体外研究 Ertugliflozin (PF-04971729) demonstrates 2000-fold selectivity for SGLT2 inhibition (relative to SGLT1) invitro 3.体内研究 Ertugliflozin (PF-04971729) reveals a concentration-dependent glucosuria after oral administration to rats 3.户使本产品发表的

6、科研献 Biochem Pharmacol. 2016 Feb 1;101:27-39.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Mascitti V, et al. Discovery of a clinical candidate from the structurally unique dioxa-bicyclo3.2.1octane class of sodium-dependentglucose cotransporter 2 inhibitors. J Med Chem. 2011 A

7、pr 28;54(8):2952-60.2. Miao Z, et al. Pharmacokinetics, metabolism, and excretion of the antidiabetic agent ertugliflozin (PF-04971729) in healthy malesubjects. 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 glucosecotransporter 2 and clinical candidate for the treatment of type 2 diabetes mellitus. Drug Metab Dispos. 2011 Sep;39(9):1609-19.McePdfHeightCaution: Product has not been fully validated for medical applications.For re