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Empagliflozin

Catalog No. T1766   CAS 864070-44-0
Synonyms: BI 10773

Empagliflozin (BI 10773) is an SGLT-2 inhibitor (IC50=3.1 nM) that is potent and selective, with more than 300-fold selectivity for SGLT-1/4/5/6. Empagliflozin is used for the treatment of type 2 diabetes.

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Empagliflozin Chemical Structure
Empagliflozin, CAS 864070-44-0
Pack Size Availability Price/USD Quantity
5 mg In stock $ 39.00
10 mg In stock $ 55.00
50 mg In stock $ 72.00
100 mg In stock $ 97.00
200 mg In stock $ 147.00
500 mg In stock $ 198.00
1 g In stock $ 372.00
5 g In stock $ 888.00
10 g In stock $ 1,230.00
1 mL * 10 mM (in DMSO) In stock $ 43.00
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Purity: 99.89%
Purity: 99.86%
Purity: 99.86%
Purity: 98.32%
Purity: 98%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Empagliflozin (BI 10773) is an SGLT-2 inhibitor (IC50=3.1 nM) that is potent and selective, with more than 300-fold selectivity for SGLT-1/4/5/6. Empagliflozin is used for the treatment of type 2 diabetes.
Targets&IC50 SGLT2:3.1 nM
In vitro In kinetic binding experiments, [3H]-Empagliflozin exhibited high affinity for SGLT-2 in the absence of glucose, demonstrating an average Kd of 57 nM and a half-life of binding to SGLT-2 of 59 minutes. Empagliflozin competitively binds to SGLT-2 against glucose. The selectivity of Empagliflozin for hSGLT-2 was substantially higher compared to other glucose transporters: 2500 times greater than hSGLT-1 (IC50 8300 nM), over 3500 times that of hSGLT-4, more than 350 times that of hSGLT-5 (IC50 = 1100 nM), and over 600 times that of hSGLT-6. Additionally, at a concentration of 10 μM, Empagliflozin did not inhibit GLUT1.
In vivo Long-term treatment with Empagliflozin can improve blood glucose control and characteristics of metabolic syndrome in diabetic rats. After treating dogs with 5 mg/kg Empagliflozin for 24 hours, plasma concentrations were over 100 times higher than the measured IC50 value. The total plasma clearance rate for Empagliflozin in ZDF rats was 43 mL/min/kg, compared to 1.8 mL/min/kg in dogs. The Cmax for ZDF rats and dogs treated with Empagliflozin were respectively 167 nM and 17254 nM. Additionally, the bioavailability of Empagliflozin in ZDF rats was 33.2%, whereas it reached up to 89.0% in dogs.
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 MTS assay(Only for Reference)
Synonyms BI 10773
Molecular Weight 450.91
Formula C23H27ClO7
CAS No. 864070-44-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 83 mg/mL (184.1 mM)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

TargetMolReferences and Literature

1. Mihaljević V, et al. Molecular Mechanisms Linking Empagliflozin to Renal Protection in the LLC-PK1 Model of Diabetic Nephropathy. Biomedicines. 2022 Nov 20;10(11):2983. 2. Lee WC, et al. Empagliflozin Protects HK-2 Cells from High Glucose-Mediated Injuries via a Mitochondrial Mechanism. Cells. 2019 Sep 14;8(9):1085. 3. Li C, et al. SGLT2 inhibition with empagliflozin attenuates myocardial oxidative stress and fibrosis in diabetic mice heart. Cardiovasc Diabetol. 2019 Feb 2;18(1):15. 4. Cheng ST, et al. The Effects of Empagliflozin, an SGLT2 Inhibitor, on Pancreatic β-Cell Mass and Glucose Homeostasis in Type 1 Diabetes. PLoS One. 2016 Jan 25;11(1):e0147391. 6. Sakaeda T, et al. Susceptibility to serious skin and subcutaneous tissue disorders and skin tissue distribution of sodium-dependent glucose co-transporter type 2 (SGLT2) inhibitors. Int J Med Sci. 2018 Jun 13;15(9):937-943. 7. Kim P, Kim G Y, Cho M Y, et al. Manufacture and Characterization of Two Distinct Quasi-polymorphs of Empagliflozin[J]. Journal of Crystal Growth. 2020: 125489.

TargetMolCitations

1. Tian G, Yu Y, Deng H, et al. Empagliflozin alleviates ethanol‐induced cardiomyocyte injury through inhibition of mitochondrial apoptosis via a SIRT1/PTEN/Akt pathway. Clinical and Experimental Pharmacology and Physiology. 2021, 48(6): 837-845. 2. Kim P, Kim G Y, Cho M Y, et al. Manufacture and Characterization of Two Distinct Quasi-polymorphs of Empagliflozin. Journal of Crystal Growth. 2020: 125489

Related compound libraries

This product is contained In the following compound libraries:
Highly Selective Inhibitor Library Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library Anti-Cancer Approved Drug Library FDA-Approved & Pharmacopeia Drug Library GPCR Compound Library FDA-Approved Drug Library Glutamine Metabolism Compound Library Glycometabolism Compound Library Anti-Cardiovascular Disease Compound Library

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Keywords

Empagliflozin 864070-44-0 GPCR/G Protein SGLT BI-10773 BI 10773 inhibit Inhibitor Sodium-dependent glucose cotransporters BI10773 inhibitor

 

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