[CAS NO. 864070-44-0]  Empagliflozin

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PRODUCTS SPECIFICATIONS [864070-44-0]

Distributor
Catalog
HY-15409
Brand
MCE
CAS
864070-44-0

DESCRIPTION [864070-44-0]

Overview

MDLMFCD22566222
Molecular Weight450.91
Molecular FormulaC23H27ClO7
SMILESClC(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

For research use only. We do not sell to patients.

41 Publications Citing Use of MCE


Summary

Empagliflozin (BI 107730 is a selective sodium glucose cotransporter-2 ( SGLT-2 ) inhibitor with an IC 50 of 3.1 nM for human SGLT-2 [1] .


IC50 & 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) [1]


In Vitro

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 [ 14 C]-alpha-methyl glucopyranoside (AMG) via hSGLT-2 in a dose-dependent manner with an IC 50 of 3.1 nM, but is less potent for other SGLTs (IC 50 range: 1100-11000 nM). [ 3 H]-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] .

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


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] .

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


Clinical Trial

NCT Number Sponsor Condition Start Date Phase
NCT04796428 Center for Outcomes Research and Clinical Epidemiology, Italy|Italian Society of Diabetology
Diabetes Mellitus, Type 2
June 30, 2021 Phase 4
NCT04345796 Asan Medical Center|Chong Kun Dang Pharmaceutical Company
Tricuspid Regurgitation|Right Ventricular Dilatation
February 15, 2021 Phase 3
NCT04937816 Boehringer Ingelheim
Diabetes Mellitus, Type 2
June 1, 2021

Appearance

Solid


Shipping

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

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL ( 110.89 mM ; Need ultrasonic)

H 2 O : 0.11 mg/mL ( 0.24 mM ; Need ultrasonic and warming)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2177 mL 11.0887 mL 22.1774 mL
5 mM 0.4435 mL 2.2177 mL 4.4355 mL
10 mM 0.2218 mL 1.1089 mL 2.2177 mL
* Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one: 0.5%HPMC

    Solubility: 5 mg/mL (11.09 mM); Suspension solution; Need ultrasonic

  • 2.

    Add each solvent one by one: 5% DMSO >> 40% PEG300 >> 5% Tween-80 >> 50% saline

    Solubility: ≥ 2.87 mg/mL (6.36 mM); Clear solution

  • 3.

    Add each solvent one by one: 5% DMSO >> 95% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.87 mg/mL (6.36 mM); Clear solution

  • 4.

    Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

    Solubility: ≥ 2.08 mg/mL (4.61 mM); Clear solution

  • 5.

    Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (4.61 mM); Clear solution

  • 6.

    Add each solvent one by one: 10% DMSO >> 90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.61 mM); Clear solution

* All of the co-solvents are available by MCE.


Synonyms

D-Glucitol, 1,5-anhydro-1-C-[4-chloro-3-[[4-[[(3S)-tetrahydro-3-furanyl]oxy]phenyl]methyl]phenyl]-, (1S)-
(1S)-1,5-Anhydro-1-C-[4-chloro-3-[[4-[[(3S)-tetrahydro-3-furanyl]oxy]phenyl]methyl]phenyl]-D-glucitol
Empagliflozin
BI 10773
Jardiance