
Empagliflozin NEW
Price | $39 | $55 | $72 |
Package | 5mg | 10mg | 50mg |
Min. Order: | |
Supply Ability: | 10g |
Update Time: | 2025-06-23 |
Product Details
Product Name: Empagliflozin | CAS No.: 864070-44-0 |
Purity: 99.89% | Supply Ability: 10g |
Release date: 2025/06/23 |
Product Introduction
Bioactivity
Name | Empagliflozin |
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. |
Cell Research | MTS assay(Only for Reference) |
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. |
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. |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice./Shipping at ambient temperature. |
Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 8.3 mg/mL (18.41 mM), Solution. DMSO : 55 mg/mL (121.98 mM), Sonication is recommended. Ethanol : < 1 mg/mL (insoluble or slightly soluble) |
Keywords | Sodium-dependent glucose cotransporters | SGLT6 | SGLT5 | SGLT4 | SGLT2 | SGLT1 | SGLT | Inhibitor | inhibit | Empagliflozin | BI-10773 | BI10773 |
Inhibitors Related | Dapagliflozin ((2S)-1,2-propanediol, hydrate) | Ertugliflozin L-pyroglutamic acid | Dapagliflozin | Ipragliflozin | Sotagliflozin | Canagliflozin hemihydrate | Tofogliflozin (hydrate) | Phlorizin | Phloretin | Sergliflozin A | Canagliflozin | Ertugliflozin |
Related Compound Libraries | Highly Selective Inhibitor Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | EMA Approved Drug Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | FDA-Approved Drug Library | Anti-Cancer Approved Drug Library | Bioactive Compounds Library Max | GPCR Compound Library | Anti-Cancer Drug Library |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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- Since: 2011-01-07
- Address: 36 Washington Street, Wellesley Hill, MA
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