Empagliflozin (BI 10773)

Catalog No.S8022

Empagliflozin (BI 10773) Chemical Structure

Molecular Weight(MW): 450.91

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.

Size Price Stock Quantity  
In DMSO USD 490 In stock
USD 270 In stock
USD 870 In stock
Bulk Discount

Free Overnight Delivery on orders over $ 500
Next day delivery by 10:00 a.m. Order now.

Purity & Quality Control

Choose Selective SGLT Inhibitors

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]

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

Kinase Assay:[1]
+ Expand

[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]
+ Expand
  • Cell lines: HK2 cells (human kidney PTC line)
  • Concentrations: ~ 500 nM
  • Incubation Time: 72 h
  • Method: MTS assay
    (Only for Reference)
Animal Research:[1]
+ Expand
  • Animal Models: ZDF rats and beagle dogs
  • Formulation: 4.4% HP-β-cyclodextrin in normal saline (intravenously) or 0.5% hydroxyethylcellulose (orally)
  • Dosages: ~2 mL/kg
  • Administration: Intravenously or orally
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 90 mg/mL (199.59 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents individually and in order:
15% Captisol
15 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 450.91
Formula

C23H27ClO7

CAS No. 864070-44-0
Storage powder
Synonyms N/A

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03027960 Not yet recruiting Heart Failure|Type II; Diabetes Yale University|Boehringer Ingelheim February 28, 2017 Phase 2
NCT02768220 Not yet recruiting SGLT-2 Inhibitors|Advanced Glycation End Products|Diabetes Northwell Health July 2017 Phase 4
NCT03008551 Not yet recruiting Polycystic Ovary Syndrome University of Hull March 2017 Phase 2|Phase 3
NCT03030222 Not yet recruiting Heart Failure Saint Lukes Health System March 2017 Phase 4
NCT02998970 Recruiting Diabetes|Cardiovascular Disease St. Michaels Hospital, Toronto|Boehringer Ingelheim (Canada) LTD January 2017 Phase 4
NCT03050229 Recruiting Nocturnal Hypertension|T2DM (Type 2 Diabetes Mellitus) Jichi Medical University|Boehringer Ingelheim|Eli Lilly and Company January 2017 Phase 4

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.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

SGLT Signaling Pathway Map

Related SGLT Products

Tags: buy Empagliflozin (BI 10773) | Empagliflozin (BI 10773) supplier | purchase Empagliflozin (BI 10773) | Empagliflozin (BI 10773) cost | Empagliflozin (BI 10773) manufacturer | order Empagliflozin (BI 10773) | Empagliflozin (BI 10773) distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID