Name: BI-10773 (Empagliflozin)
Brand: Selleck Chemicals
SKU: S8022
Availability: InStock
Rating: 5 (30 reviews)

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Quality Control

Batch: Purity: 99.97%

99.97

Related Targets	CXCR Hedgehog/Smoothened PKA Adrenergic Receptor AChR 5-HT Receptor Histamine Receptor Dopamine Receptor Ras KRas
Other SGLT Inhibitors	Sotagliflozin (LX4211) Phlorizin Phloretin (RJC 02792) Tofogliflozin(CSG 452) Ipragliflozin L-Proline Ipragliflozin (ASP1941) Swertisin KGA-2727 Mizagliflozin (KWA 0711) Bexagliflozin (EGT1442)

Cell Culture, Treatment & Working Concentration

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
Click to View More Cell Line Experimental Data

Solubility

In vitro
Batch:

DMSO : 90 mg/mL (199.59 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	15% Captisol Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	10.000mg/ml (22.18mM)	Taking the 1 mL working solution as an example, take 10 mg of this product, add it to 1 ml of 15% Captisol clear solution, and mix evenly to form a uniform suspension. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5% DMSO 1 40% PEG 300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	4.500mg/ml (9.98mM)	Taking the 1 mL working solution as an example, add 50 μL of 90 mg/mL clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify; add 50 μL of Tween-80 to the above system, mix evenly to clarify; Then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

%

% Tween 80

% ddH₂O

% DMSO

+

%

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	450.91	Formula	C₂₃H₂₇ClO₇	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	864070-44-0	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	BI 10773			Smiles	C1COCC1OC2=CC=C(C=C2)CC3=C(C=CC(=C3)C4C(C(C(C(O4)CO)O)O)O)Cl

Mechanism of Action

Targets/IC₅₀/Ki	SGLT2 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 of this compound. In kinetic binding experiments, [³H]-empagliflozin displays a high affinity for SGLT-2 with a mean K_d 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.
Kinase Assay	[¹⁴C]-monosaccharide uptake inhibition experiments
Kinase Assay	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 this 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 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 this compound. The total plasma clearance of this chemical in ZDF rat is 43 mL/min/kg, while in dogs is lower at 1.8 mL/min/kg. C_max of this agent in ZDF rat and dogs is 167 nM and 17254 nM, respectively. Terminal elimination half-life in ZDF rat and dogs is 1.5 h and 6.3 h, respectively. Bioavailability of this drug in ZDF rat is 33.2%, while in dogs is higher at 89.0%. Long-term treatment with this medication, improves glycaemic control and features of metabolic syndrome in diabetic rats.
References	[1] https://pubmed.ncbi.nlm.nih.gov/21985634/ [2] https://pubmed.ncbi.nlm.nih.gov/21985693/ [3] https://pubmed.ncbi.nlm.nih.gov/23390498/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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BI-10773 (Empagliflozin) SGLT2 inhibitor

Chemical Structure

Molecular Weight: 450.91