Empagliflozin (BI 107730 is a selective sodium glucose cotransporter-2 (SGLT-2) inhibitor with an IC₅₀ of 3.1 nM for human SGLT-2^[1].

Empagliflozin is a potent and competitive SGLT-2 inhibitor with an excellent selectivity profile and the highest selectivity window of the tested SGLT-2 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 for other SGLTs (IC₅₀ range: 1100-11000 nM). [³H]-Empagliflozin displays a high affinity for SGLT-2 with a mean K_d of 57±37 nM in the absence of glucose in kinetic binding experiments^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Glucose intolerance is significantly improved after 8 days of Empagliflozin treatment at either dose (3mg/kg Empagliflozin 3058±180 vs 10mg/kg Empagliflozin 3090±219). Therefore, acute treatment with Empagliflozin has a beneficial effect on hyperglycemia and glucose intolerance. Since there are no significant differences in blood glucose homeostasis with the two different doses of Empagliflozin, and random blood glucose levels of T1DM mice are significantly improved by 3mg/kg of Empagliflozin, the effect of the lower dose of Empagliflozin (3mg/kg) is investigated on preserving β-cell mass and function^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

450.91

C₂₃H₂₇ClO₇

864070-44-0

Solid

White to off-white

ClC(C=CC([C@@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O)=C2)=C2CC(C=C3)=CC=C3O[C@H]4CCOC4

Room temperature in continental US; may vary elsewhere.

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

• [1]. Grempler R, et al. Empagliflozin, a novel selective sodium glucose cotransporter-2 (SGLT-2) inhibitor: characterisation and comparison with other SGLT-2 inhibitors. Diabetes Obes Metab. 2012 Jan;14(1):83-90.  [Content Brief]

  [2]. Cheng ST, et al. The Effects of Empagliflozin, an SGLT2 Inhibitor, on Pancreatic β-Cell Mass and Glucose Homeostasis in Type 1 Diabetes. PLoS One. 2016 Jan 25;11(1):e0147391.  [Content Brief]

  [3]. Nikole J.ByrneBSc, et al. Empagliflozin Prevents 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.  [Content Brief]