Empagliflozin_product_DataBase

Bioactivity

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].

Target

IC50: 3.1 nM (SGLT-2), 1.1 μM (SGLT-5), 2 μM (SGLT-6), 8.3 μM (SGLT-1), 11 μM (SGLT-4)

Invitro

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 Kd of 57±37 nM in the absence of glucose in kinetic binding experiments[1].

In Vivo

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].

Name

Empagliflozin

CAS

864070-44-0

Formula

C23H27ClO7

Molar Mass

450.91

Appearance

Solid

Transport

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Reference

[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. [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. [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.

PeptideDB

Empagliflozin

CAS: 864070-44-0 F: C23H27ClO7 W: 450.91