恩格列净作用机制 - Medchemexpress - MCE中国

1、Product Data SheetEmpagliflozinCat. No.: HY-15409CAS No.: 864070-44-0分式: CHClO分量: 450.91作靶点: SGLT作通路: Membrane Transporter/Ion Channel储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 250 mg/mL (554.43 mM; Need ultrasonic)H2O : 0.11 mg/mL (0.24 mM; Need ultrasoni

2、c and warming)SolventMass1 mg 5 mg 10 mgConcentration制备储备液1 mM 2.2177 mL 11.0887 mL 22.1774 mL5 mM 0.4435 mL 2.2177 mL 4.4355 mL10 mM 0.2218 mL 1.1089 mL 2.2177 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；旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存式和期限：-80C, 6 months; -20C, 1 month。-80C 储存时，请在 6 个内使，-20C 储存时，请在 1 个内使。体内实验请根

3、据您的实验动物和给药式选择适当的溶解案。以下溶解案都请先按照 In Vitro 式配制澄清的储备液，再依次添加助溶剂：为保证实验结果的可靠性，澄 的储备液可以根据储存条件，适当保存；体内实验的作液，建议您现现配，当天使； 以下溶剂前显的百分 指该溶剂在您配制终溶液中的体积占；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的式助溶1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (4.61 mM); Clear solution此案可获得 2.08 mg/mL (4.61 mM，

4、饱和度未知) 的澄清溶液。以 1 mL 作液为例，取 100 L 20.8 mg/mL 的澄 DMSO 储备液加到 400 L PEG300 中，混合均匀；向上述体系中加50 L Tween-80，混合均匀；然后继续加 450 L 理盐定容 1 mL。2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.08 mg/mL (4.61 mM); Clear solutionPage 1 of 2 www.MedChemE此案可获得 2.08 mg/mL (4.61 mM，饱和度未知) 的澄清溶液。以 1 mL 作液为例，取

5、100 L 20.8 mg/mL 的澄 DMSO 储备液加到 900 L 20% 的 SBE-CD 理盐溶液中，混合均匀。3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.08 mg/mL (4.61 mM); Clear solution此案可获得 2.08 mg/mL (4.61 mM，饱和度未知) 的澄 溶液，此案不适于实验周 期在半个以上的实验。以 1 mL 作液为例，取 100 L 20.8 mg/mL 的澄 DMSO 储备液加到 900 L 油中，混合均匀。BIOLOGICAL ACTIVITY物活性 Empagliflozin种选择

6、性钠葡萄糖协同转运蛋-2 (SGLT-2) 抑制剂，抑制SGLT-2的IC50 为3.1 nM。IC & Target IC50: 3.1 nM (SGLT-2), 1.1 M (SGLT-5), 2 M (SGLT-6), 8.3 M (SGLT-1), 11 M (SGLT-4)1体外研究 Empagliflozin is a potent and competitive SGLT-2 inhibitor with an excellent selectivity profile and the highestselectivity window of the tested SGLT-2

7、inhibitors over hSGLT-1. Empagliflozin inhibits the uptake of 14C-alpha-methyl glucopyranoside (AMG) via hSGLT-2 in a dose-dependent manner with an IC50 of 3.1 nM, but is less potent forother SGLTs (IC50 range: 1100-11000 nM). 3H-Empagliflozin displays a high affinity for SGLT-2 with a mean Kd of573

8、7 nM in the absence of glucose in kinetic binding experiments1.体内研究 Glucose intolerance is significantly improved after 8 days of Empagliflozin treatment at either dose (3mg/kg Empagliflozin 3058180 vs 10mg/kg Empagliflozin 3090219). Therefore, acute treatment with Empagliflozin has a beneficial eff

9、ect on hyperglycemia and glucose intolerance. Since there are no significant differences in blood glucosehomeostasis with the two different doses of Empagliflozin, and random blood glucose levels of T1DM mice aresignificantly improved by 3mg/kg of Empagliflozin, the effect of the lower dose of Empag

10、liflozin (3mg/kg) isinvestigated on preserving -cell mass and function2.PROTOCOLAnimal Mice2Administration 2 Male C57BL/6J mice (10 weeks of age) are used. Empagliflozin is dissolved in hydroxy ethyl cellulose (HEC) andadministered to mice in the experimental group (3 or 10 mg/kg) by oral gavage onc

11、e daily for 8 days, whereas thevehicle group is given same volume of HEC alone.MCE has not independently confirmed the accuracy of these methods. They are for reference only.户使本产品发表的科研献 Diabetologia. 2017 Mar;60(3):568-573. Cell Physiol Biochem. 2019 Nov. Biochem Pharmacol. 2018 Jun;152:45-59. Mol C

12、ell Endocrinol. 2019 Jun 10:110487. Life Sci. 2019 Jul 1:116622.See more customer validations on HYPERLINK www.MedChemE www.MedChemEPage 2 of 3 www.MedChemEREFERENCES1. Grempler R, et al. Empagliflozin, a novel selective sodium glucose cotransporter-2 (SGLT-2) inhibitor: characterisation and compari

13、son with other SGLT-2inhibitors. Diabetes Obes Metab. 2012 Jan;14(1):83-90.2. Cheng ST, et al. The Effects of Empagliflozin, an SGLT2 Inhibitor, on Pancreatic -Cell Mass and Glucose Homeostasis in Type 1 Diabetes. PLoS One. 2016Jan 25;11(1):e0147391.3. Nikole J.ByrneBSc, et al. Empagliflozin Prevent

14、s Worsening of Cardiac Function in an Experimental Model of Pressure Overload-Induced Heart Failure.JACC Basic Transl Sci. 2017 Aug;2(4):347-354.4. Sakaeda T, et al. Susceptibility to serious skin and subcutaneous tissue disorders and skin tissue distribution of sodium-dependent glucose co-transporter type 2 (SGLT2) inhibitors. Int J Med Sci. 2018 Jun 13;15(9):937-943.McePdfHe