Empagliflozin

SKU: orb1307498

Description

Empagliflozin

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 864070-44-0
• MW: 450.91
• Purity: 99.98%
• Formula: C₂₃H₂₇ClO₇
• SMILES: O[C@H]1[C@H](C2=CC(CC3=CC=C(O[C@H]4CCOC4)C=C3)=C(Cl)C=C2)O[C@H](CO)[C@@H](O)[C@@H]1O
• Target: SGLT
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:8.3 mg/mL (18.41 mM);DMSO:242.5 mg/mL (537.8 mM);Ethanol:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

• Target IC50:
  SGLT1:8.3 μM|SGLT2:57 ± 37 nM (Kd)|SGLT5:1.1 μM|SGLT2:3.1 nM|SGLT4:11 μM|SGLT6:2 μM
• 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.
• 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.
• Cell Research:
  MTS assay(Only for Reference)

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

inhibit, Inhibitor, Empagliflozin, BI10773, BI-10773, BI 10773, SGLT6, SGLT4, SGLT5, SGLT, SGLT1, SGLT2, Sodium-dependent glucose cotransporters

Compound Identifiers

PubChem CID

11949646