Empagliflozin (BI 10773)

For research use only.

Catalog No.S8022

12 publications

Empagliflozin (BI 10773) Chemical Structure

CAS No. 864070-44-0

Empagliflozin (BI-10773) is a potent and selective SGLT-2 inhibitor with IC50 of 3.1 nM, exhibits >300-fold selectivity over SGLT-1, 4, 5 and 6. Phase 3.

Selleck's Empagliflozin (BI 10773) has been cited by 12 publications

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  • Effects of empagliflozin on AMPK/ACC phosphorylation

    Diabetes, 2016, 65(9):2784-94. Empagliflozin (BI 10773) purchased from Selleck.

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Biological Activity

Description Empagliflozin (BI-10773) is a potent and selective SGLT-2 inhibitor with IC50 of 3.1 nM, exhibits >300-fold selectivity over SGLT-1, 4, 5 and 6. Phase 3.
SGLT2 [1]
3.1 nM
In vitro

Empagliflozin shows >2500-fold selectivity for hSGLT-2 over hSGLT-1 (IC50 8300 nM) and >3500-fold selectivity over hSGLT-4, it exhibits >350-fold selectivity over hSGLT-5 (IC50=1100 nM) and >600-fold selectivity over hSGLT-6. No relevant inhibition of GLUT1 is observed up to 10 μM Empagliflozin. In a kinetic binding experiments, [3H]-empagliflozin displays a high affinity for SGLT-2 with a mean Kd of 57 nM in the absence of glucose, and shows a half-life of [3H]-empagliflozin-binding to SGLT-2 of 59 min in the absence of glucose.Its binding to SGLT-2 is competitive with glucose. [1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HEK293 MnXpSpVv[3Srb36gZZN{[Xl? MUOxOUBucW6| M{fhSGlvcGmkaYTpc44hd2ZicnXjc41jcW6jboSgbJVu[W5iU1fMWFIh\XiycnXzd4VlKGmwIFjFT|I6OyClZXzsd{Bie3Onc4Pl[EBieyCmZXPy[YF{\SCrbjDbNVREZS2DTVegeZB1[WunIIDy[Ylv[3WkYYTl[EBnd3JiMUWgcYlveyCob3zsc5dm\CCkeTDbNVREZS2DTVegZYRlcXSrb36gZY5lKG2nYYP1doVlKGGodHXyJFQhcHK|IHL5JHRweGOxdX70JI1mfGixZDygTWM2OCB;IECuNFA{OSEQvF2u MmDVQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlExPzh|MD:nQmNpTU2ETEyvZV4>

... Click to View More Cell Line Experimental Data

In vivo High exposure of empagliflozin is achieved in dogs, with plasma concentrations >100-fold above IC50 measured 24 h after administration of 5 mg/kg empagliflozin. The total plasma clearance of empagliflozin in ZDF rat is 43 mL/min/kg, while in dogs is lower at 1.8 mL/min/kg. Cmax of empagliflozin in ZDF rat and dogs is 167 nM and 17254 nM, respectively. [1] Terminal elimination half-life in ZDF rat and dogs is 1.5 h and 6.3 h, respectively. Bioavailability of empagliflozin in ZDF rat is 33.2%, while in dogs is higher at 89.0%. Long-term treatment with empagliflozin, improves glycaemic control and features of metabolic syndrome in diabetic rats. [2]


Kinase Assay:[1]
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[14C]-monosaccharide uptake inhibition experiments:

Stable cell lines over-expressing hSGLT-1, -2, -4, -5 or -6 or rSGLT-1 or -2 are used for the sodium-dependent monosaccharide transport inhibition assay. Cells are pre-incubated in 200 μL uptake buffer (10 mM HEPES, 137 mM NaCl, 5.4 mM KCl, 2.8 mM CaCl2, 1.2 mM MgCl2, 50 μg/ml Gentamycin, 0.1% BSA) for 25 minutes at 37°C. 10 μM Cytochalasin B and test compound is added at different concentrations 15 minutes before the initiation of the uptake experiment. The uptake reaction is started by the addition of 0.6 μCi [14C]-labelled monosaccharide i.e. [14C]-labelled AMG, glucose, fructose, mannose or myo-inositol, in 0.1 mM AMG (or the respective non-radioactive monosaccharide). After incubation for 60 minutes (hSGLT-5), 90 minutes (hSGLT-4) or 4 hours (hSGLT-2) at 37°C, the cells are washed three times with 300 μL PBS and then lysed in 0.1 N NaOH with intermittent shaking for 5 minutes. The lysate is mixed with 200 μL MicroScint 40 and shaken for 15 minutes and counted for radioactivity in the TopCount NXT. For SGLT-4 and SGLT-5 assays cells are pre-incubated in pre-treatment buffer (uptake buffer containing choline chloride instead of NaCl) for 25 minutes prior to addition of uptake buffer.
Cell Research:[3]
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  • Cell lines: HK2 cells (human kidney PTC line)
  • Concentrations: ~ 500 nM
  • Incubation Time: 72 h
  • Method: MTS assay
    (Only for Reference)
Animal Research:[1]
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  • Animal Models: ZDF rats and beagle dogs
  • Dosages: ~2 mL/kg
  • Administration: Intravenously or orally
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 90 mg/mL (199.59 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
15% Captisol
For best results, use promptly after mixing.
15 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 450.91


CAS No. 864070-44-0
Storage powder
in solvent
Synonyms N/A
Smiles C1COCC1OC2=CC=C(C=C2)CC3=C(C=CC(=C3)C4C(C(C(C(O4)CO)O)O)O)Cl

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04986735 Recruiting Drug: Empagliflozin Glycogen Storage Disease Type IB Hong Kong Children''s Hospital August 8 2021 --
NCT04911660 Not yet recruiting Drug: Empagliflozin 25 MG|Other: Placebo Kidney Stone University Hospital Inselspital Berne|Boehringer Ingelheim|University of Bern June 2021 Phase 2
NCT04702490 Active not recruiting Drug: MET409 Active|Drug: MET409 Placebo|Drug: Empagliflozin NASH|NASH - Nonalcoholic Steatohepatitis|Type 2 Diabetes|Diabetes Type 2|Diabetes|Fatty Liver|Fatty Liver Nonalcoholic|NAFLD Metacrine Inc. December 15 2020 Phase 2
NCT04450563 Recruiting Drug: 14-day outpatient intervention Type 1 Diabetes McGill University November 2 2020 Phase 1

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID