1. Membrane Transporter/Ion Channel
  2. SGLT

Empagliflozin (Synonyms: BI 10773)

Cat. No.: HY-15409 Purity: 99.91% ee.: 98.83%
Data Sheet SDS Handling Instructions

Empagliflozin is a selective sodium glucose cotransporter-2 (SGLT-2) inhibitor with an IC50 of 3.1 nM for hSGLT-2.

For research use only. We do not sell to patients.
Empagliflozin Chemical Structure

Empagliflozin Chemical Structure

CAS No. : 864070-44-0

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10 mM * 1 mL in DMSO $55 In-stock
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10 mg $70 In-stock
50 mg $170 In-stock
100 mg $270 In-stock
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    Empagliflozin purchased from MCE. Usage Cited in: JACC Basic Transl Sci. 2017 Aug;2(3):347-354.

    Improved In Vivo Cardiac Function in Empagliflozin-Treated Mice With Heart Failure Is PreservedEx Vivo. Hearts from vehicle- and Empa-treated mice with HF are perfused ex vivo to measure cardiac function. Cardiac output (A) and cardiac work (B) are measured using ex vivo perfused working hearts.

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    • Biological Activity

    • Protocol

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    • Purity & Documentation

    • References

    Description

    Empagliflozin is a selective sodium glucose cotransporter-2 (SGLT-2) inhibitor with an IC50 of 3.1 nM for hSGLT-2.

    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 [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].

    Clinical Trial
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    References
    Preparing Stock Solutions
    Concentration Volume 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.
    Kinase Assay
    [1]

    Membranes (60 μg/well) are assayed in a 10 mM 4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid (HEPES) buffer (pH 7.4) containing 137 mM NaCl in the presence or absence of 20 mM glucose and indicated concentrations of [3H]-Empagliflozin in 96-well plates at room temperature for 2 h. Incubations are stopped by rapid filtration through GF/B Filterplates impregnated with polyethyleneimine 0.5% and prewetted with 0.9% NaCl solution, and washed four times with 0.9% NaCl solution (4°C) using a Harvester Filtermate 96. Filterplates are dried for 2 h and 50 μL of Microscint 20 is added to each well. Radioactivity retained on the filters is measured using the TopCount NXT. In parallel, the actual amount of activity used in the assays is determined by adding the same amount of [3H]-Empagliflozin that is added per well in the radioligand binding studies and 4 mL Ultima Gold Scintilator into 5 mL vials and measuring using a Tricarb 2900TR. Non-specific [3H]-Empagliflozin-binding is determined in the presence of 30 μM dapagliflozin[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [2]

    Empagliflozin is dissolved in hydroxy ethyl cellulose (HEC) (Mice)[2].

    Mice[2]
    Male C57BL/6J mice (10 weeks of age) are used. Empagliflozin is dissolved in hydroxy ethyl cellulose (HEC) and administered to mice in the experimental group (3 or 10 mg/kg) by oral gavage once daily for 8 days, whereas the vehicle group is given same volume of HEC alone. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    450.91

    Formula

    C₂₃H₂₇ClO₇

    CAS No.

    864070-44-0

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

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    10 mM in DMSO

    Empagliflozin is preppared in 0.5% hydroxyethyl cellulose[3].

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

    References

    Purity: 99.91% ee.: 98.83%

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    Product Name:
    Empagliflozin
    Cat. No.:
    HY-15409
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