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Empagliflozin (BI 10773)

SGLT-2 inhibitor for oral treatment of type 2 diabetes CAS# 864070-44-0

Empagliflozin (BI 10773)

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Chemical Properties of Empagliflozin (BI 10773)

Cas No. 864070-44-0 SDF Download SDF
PubChem ID 11949646 Appearance Powder
Formula C23H27ClO7 M.Wt 450.91
Type of Compound N/A Storage Desiccate at -20°C
Synonyms BI 10773
Solubility DMSO : 250 mg/mL (554.43 mM; Need ultrasonic)
H2O : 0.11 mg/mL (0.24 mM; Need ultrasonic and warming)
Chemical Name (2S,3R,4R,5S,6R)-2-[4-chloro-3-[[4-[(3S)-oxolan-3-yl]oxyphenyl]methyl]phenyl]-6-(hydroxymethyl)oxane-3,4,5-triol
SMILES C1COCC1OC2=CC=C(C=C2)CC3=C(C=CC(=C3)C4C(C(C(C(O4)CO)O)O)O)Cl
Standard InChIKey OBWASQILIWPZMG-QZMOQZSNSA-N
Standard InChI InChI=1S/C23H27ClO7/c24-18-6-3-14(23-22(28)21(27)20(26)19(11-25)31-23)10-15(18)9-13-1-4-16(5-2-13)30-17-7-8-29-12-17/h1-6,10,17,19-23,25-28H,7-9,11-12H2/t17-,19+,20+,21-,22+,23-/m0/s1
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of Empagliflozin (BI 10773)

DescriptionEmpagliflozin (BI 10773) is a selective, potent and dose-depentent inhibitor of SGLT-2(sodium glucose cotransporter-2) with IC50 values of 3.1 nM, 8300 nM, 11000 nM, 1100 nM and 2000 nM, for SGLT-2,1,4,5 and 6, respectively.
TargetsSGLT-2    
IC503.1 nM     

Protocol

Kinase Assay [1]
Membranes (60 μg/well) are assayed in a 10 mM 4-(2-hydroxyethyl)-1-piperazineethanesulfonic acid (HEPES) buffer (pH 7.4) containing 137 mM NaCl in the presence or absence of 20 mM glucose and indicated concentrations of [3H]-Empagliflozin in 96-well plates at room temperature for 2 h. Incubations are stopped by rapid filtration through GF/B Filterplates impregnated with polyethyleneimine 0.5% and prewetted with 0.9% NaCl solution, and washed four times with 0.9% NaCl solution (4°C) using a Harvester Filtermate 96. Filterplates are dried for 2 h and 50 μL of Microscint 20 is added to each well. Radioactivity retained on the filters is measured using the TopCount NXT. In parallel, the actual amount of activity used in the assays is determined by adding the same amount of [3H]-Empagliflozin that is added per well in the radioligand binding studies and 4 mL Ultima Gold Scintilator into 5 mL vials and measuring using a Tricarb 2900TR. Non-specific [3H]-Empagliflozin-binding is determined in the presence of 30 μM dapagliflozin[1].

Animal Administration [2]
Mice[2] Male C57BL/6J mice (10 weeks of age) are used. Empagliflozin is dissolved in hydroxy ethyl cellulose (HEC) and administered to mice in the experimental group (3 or 10 mg/kg) by oral gavage once daily for 8 days, whereas the vehicle group is given same volume of HEC alone.

References:
[1]. Grempler R, et al. Empagliflozin, a novel selective sodium glucose cotransporter-2 (SGLT-2) inhibitor: characterisation and comparison with other SGLT-2 inhibitors. Diabetes Obes Metab. 2012 Jan;14(1):83-90. [2]. 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. [3]. Nikole J.ByrneBSc, et al. Empagliflozin Prevents Worsening of Cardiac Function in an Experimental Model of Pressure Overload-Induced Heart Failure. JACC Basic Transl Sci. 2017 Aug;2(4):347-354. [4]. 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.

Empagliflozin (BI 10773) Dilution Calculator

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Preparing Stock Solutions of Empagliflozin (BI 10773)

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.2177 mL 11.0887 mL 22.1774 mL 44.3547 mL 55.4434 mL
5 mM 0.4435 mL 2.2177 mL 4.4355 mL 8.8709 mL 11.0887 mL
10 mM 0.2218 mL 1.1089 mL 2.2177 mL 4.4355 mL 5.5443 mL
50 mM 0.0444 mL 0.2218 mL 0.4435 mL 0.8871 mL 1.1089 mL
100 mM 0.0222 mL 0.1109 mL 0.2218 mL 0.4435 mL 0.5544 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on Empagliflozin (BI 10773)

Empagliflozin is a selective inhibitor of SGLT-2 with IC50 value of 3.1 nM [1].

Sodium glucose cotransporter-2 (SGLT-2) is a member of sodium glucose co-transporter family and plays a pivotal role in glucose reabsorption in the kidney [2].

Empagliflozin is a potent SGLT-2 inhibitor and has a high degree of selectivity over SGLT-1, 4, 5 and 6 than other reported SGLT-2 inhibitors. When tested with a panel of human cell lines over-expressed SGLT-1, 2, 4, 5 and 6, Empagliflozin treatment competitively bind to SGLT-2 over glucose at low dose [1]. In human proximal tublular cell (PTC) cell line HK2 cells, Empagliflozin treatment for 72 h inhibits the expression of SGLT-2 which in turn reversed high glucose induced TLR4 expression, NF-κB binding, IL-6 secretion, AP-1 binding and CIV expression [3].

In Zucker diabetic fatty rat model, oral administration of Empagliflozin shows good efficiency with moderate total plasma clearance (CL) and bioavailability (BA) which indicated that Empagliflozin as an innovative therapeutic approach to treat diabetes in clinic [1]. When treated Zucker diabetic fatty rat model with Empagliflozin, both single and multiple doses results in the urinary glucose excretion and reductions in blood glucose levels [4].

References:
[1].  Grempler, R., et al., Empagliflozin, a novel selective sodium glucose cotransporter-2 (SGLT-2) inhibitor: characterisation and comparison with other SGLT-2 inhibitors. Diabetes Obes Metab, 2012. 14(1): p. 83-90.
[2].  Ndefo, U.A., et al., Empagliflozin (Jardiance): A Novel SGLT2 Inhibitor for the Treatment of Type-2 Diabetes. P t, 2015. 40(6): p. 364-8.
[3].  Panchapakesan, U., et al., Effects of SGLT2 inhibition in human kidney proximal tubular cells--renoprotection in diabetic nephropathy? PLoS One, 2013. 8(2): p. e54442.
[4].   Thomas, L., et al., Long-term treatment with empagliflozin, a novel, potent and selective SGLT-2 inhibitor, improves glycaemic control and features of metabolic syndrome in diabetic rats. Diabetes Obes Metab, 2012. 14(1): p. 94-6.

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References on Empagliflozin (BI 10773)

Empagliflozin (BI 10773), a Potent and Selective SGLT2 Inhibitor, Induces Dose-Dependent Glucosuria in Healthy Subjects.[Pubmed:27121669]

Clin Pharmacol Drug Dev. 2013 Apr;2(2):152-61.

Empagliflozin is an orally available, selective inhibitor of sodium glucose cotransporter 2. In this study, single oral doses of empagliflozin from 0.5 to 800 mg were not associated with any clinically significant safety concerns in healthy male volunteers. The incidence of adverse events (AEs) was similar in subjects receiving placebo (22.2%) or empagliflozin (25.0%) in the single rising dose part of the study and after 50 mg empagliflozin under fed (28.6%) or fasted (28.6%) conditions. The most frequent AE was headache. No clinically relevant changes in laboratory or electrocardiogram (ECG) measurements were observed. Single oral doses of empagliflozin were rapidly absorbed, reaching peak levels after 1.0-2.1 hours. Increases in empagliflozin exposure were roughly dose-proportional and a dose-dependent increase in urinary glucose excretion was observed for empagliflozin doses up to 100 mg. After ingestion of 50 mg empagliflozin in conjunction with a high-fat, high-calorie meal, no clinically relevant changes in exposure were found, indicating that empagliflozin can be administered independent of food. Empagliflozin up to 800 mg did not generate clinically significant safety concerns in healthy male subjects. The pharmacokinetic properties of empagliflozin support once daily administration independent of food.

Description

Empagliflozin is a selective sodium glucose cotransporter-2 (SGLT-2) inhibitor with an IC50 of 3.1 nM for human SGLT-2.

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