Empagliflozin (BI 10773)

Catalog No.S8022

For research use only.

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.

Empagliflozin (BI 10773) Chemical Structure

CAS No. 864070-44-0

Selleck's Empagliflozin (BI 10773) has been cited by 15 publications

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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.
Targets
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 MnroSpVv[3Srb36gZZN{[Xl? NHXBPGoyPSCvaX7z NHi1[3ZKdmirYnn0bY9vKG:oIILlZ49u[mmwYX70JIh2dWGwIGPHUHQzKGW6cILld5Nm\CCrbjDISWszQTNiY3XscJMh[XO|ZYPz[YQh[XNiZHXjdoVie2ViaX6gX|E1S11vQV3HJJVxfGGtZTDwdoVqdmO3YnH0[YQh\m:{IEG1JI1qdnNiZn;scI94\WRiYomgX|E1S11vQV3HJIFl\Gm2aX;uJIFv\CCvZXHzeZJm\CCjZoTldkA1KGi{czDifUBVd3Clb4XueEBu\XSqb3SsJGlEPTBiPTCwMlAxOzFizszNMi=> NWjaU|BVRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjFyN{izNE8oRkOqRV3CUFww[T5?
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]

Protocol (from reference)

Kinase Assay:[1]
  • [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]
  • Cell lines: HK2 cells (human kidney PTC line)
  • Concentrations: ~ 500 nM
  • Incubation Time: 72 h
  • Method: MTS assay
Animal Research:[1]
  • Animal Models: ZDF rats and beagle dogs
  • Dosages: ~2 mL/kg
  • Administration: Intravenously or orally

Solubility (25°C)

In vitro

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

Chemical Information

Molecular Weight 450.91
Formula

C23H27ClO7

CAS No. 864070-44-0
Storage 3 years -20°C powder
2 years -80°C in solvent
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
NCT05139472 Recruiting Drug: Empagliflozin 10 MG Heart Failure With Preserved Ejection Fraction|Heart Failure Diastolic|Diabetes Mellitus University of Texas Southwestern Medical Center|Boehringer Ingelheim November 9 2021 Phase 3
NCT04986735 Recruiting Drug: Empagliflozin Glycogen Storage Disease Type IB Hong Kong Children''s Hospital August 8 2021 --
NCT04911660 Recruiting Drug: Empagliflozin 25 MG|Other: Placebo Kidney Stone University Hospital Inselspital Berne|Boehringer Ingelheim|University of Bern August 25 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

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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