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作靶點(diǎn): SGLT作通路: Membrane Transporter/Ion Channel儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6

2、 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 125 mg/mL (220.85 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液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請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存式和期限。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的

3、實(shí)驗(yàn)動(dòng)物和給藥式選擇適當(dāng)?shù)娜芙獍福渲魄罢?qǐng)先配制澄清的儲(chǔ)備液，再依次添加助溶劑(為保證實(shí)驗(yàn)結(jié)果的可靠性，體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使；澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (3.67 mM); Clear solution2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.08 mg/mL (3.67

4、mM); Clear solution1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemE3. 請(qǐng)依序添加每種溶劑： 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、選擇性的、具有服活性的鈉離依賴的葡萄糖協(xié)同轉(zhuǎn)運(yùn)蛋2 (SGLT2) 的有效選擇性抑制劑。其對(duì)h-SGLT2 的 IC50 值為0.877 nM 1 2

5、。 種治療2型糖尿病的臨床藥物 3。IC50 & Target IC50: 0.877 nM (h-SGLT2) 1.體外研究 Ertugliflozin (PF-04971729) demonstrates 2000-fold selectivity for SGLT2 inhibition (relative to SGLT1) invitro 3.體內(nèi)研究 Ertugliflozin (PF-04971729) reveals a concentration-dependent glucosuria after oral administration to rats 3.戶使本產(chǎn)品發(fā)表的

6、科研獻(xiàn) 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