Home GPCR & G Protein SGLT inhibitor Empagliflozin For research use only.

Empagliflozin

Synonyms: BI 10773

Empagliflozin 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 Chemical Structure

Empagliflozin Chemical Structure

CAS No. 864070-44-0

Purity & Quality Control

Empagliflozin Related Products

Signaling Pathway

SGLT Signaling Pathways

SGLT Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HEK293 Function assay 15 mins Inhibition of recombinant human SGLT2 expressed in HEK293 cells assessed as decrease in [14C]-AMG uptake preincubated for 15 mins followed by [14C]-AMG addition and measured after 4 hrs by Topcount method, IC50 = 0.0031 μM. ChEMBL
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Biological Activity

Description Empagliflozin 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
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]
Kinase Assay [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 Cell lines HK2 cells (human kidney PTC line)
Concentrations ~ 500 nM
Incubation Time 72 h
Method MTS assay
In Vivo
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]
Animal Research Animal Models ZDF rats and beagle dogs
Dosages ~2 mL/kg
Administration Intravenously or orally
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06012266 Not yet recruiting
Heart Failure
Centre Hospitalier Universitaire Vaudois|Great Ormond Street Hospital for Children NHS Foundation Trust|University College London
 August 2024 Phase 2
NCT06308679 Not yet recruiting
Healthy Vollunteer
Pharma Nueva
 May 28 2024 Phase 1
NCT06339788 Not yet recruiting
Healthy Volunteers
Handok Inc.
 April 2024 Phase 1
NCT06013865 Recruiting
Kidney Transplant|Type 2 Diabetes
VA Office of Research and Development|Iowa City VA Health Care System|VA Pittsburgh Healthcare System|Nashville VA Medical Center
 April 5 2024 Phase 4
NCT06021145 Recruiting
Type 1 Diabetes
McGill University Health Centre/Research Institute of the McGill University Health Centre|Diabetes Canada
 March 2024 Phase 4

Chemical Information & Solubility

Molecular Weight 450.91 Formula

C23H27ClO7
CAS No. 864070-44-0 SDF --
Smiles C1COCC1OC2=CC=C(C=C2)CC3=C(C=CC(=C3)C4C(C(C(C(O4)CO)O)O)O)Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 90 mg/mL ( (199.59 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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