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Empagliflozin (BI 10773) (Synonyms: BI 10773)

Catalog No.GC16212

An SGLT2 inhibitor

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Empagliflozin (BI 10773) Chemical Structure

Cas No.: 864070-44-0

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5mg
$36.00
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10mM (in 1mL DMSO)
$41.00
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10mg
$55.00
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50mg
$118.00
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100mg
$191.00
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Sample solution is provided at 25 µL, 10mM.

Product has been cited by 1 publications

Product Documents

Quality Control & SDS

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Protocol

Cell experiment [1]:

Cell lines

HK2 cells

Preparation method

The solubility of this compound in DMSO is > 20.75 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months.

Reacting condition

100 or 500 nM; 72 hrs

Applications

In HK2 cells, Empagliflozin blocked SGLT2 without causing a compensatory increase in the other glucose transporters. Empagliflozin at both concentrations significantly inhibited high glucose-induced TLR4 expression by 97.2 ± 8.2% and 64.4 ± 12.6%, respectively. Besides, at the dose of 500 nM, Empagliflozin significantly inhibited high glucose-induced NF- κB binding by 91.7 ± 14.9%. In addition, Empagliflozin reduced high glucose-induced secretion of IL-6 by 92.0 ± 11.7% and 116.5 ± 19.6% at the doses of 100 and 500 nM, respectively.

Animal experiment [2]:

Animal models

ZDF rats and beagle dogs

Dosage form

2 mL/kg; i.v. or p.o.

Applications

Empagliflozin achieved high exposure in dogs, with plasma concentrations > 100-fold above the IC50 value (measured 24 hrs after administration). In ZDF rat, the total plasma clearance of Empagliflozin was 43 mL/min/kg, while in dogs, was lower at 1.8 mL/min/kg. The Cmax values of Empagliflozin for ZDF rat and dogs were 167 nM and 17254 nM, respectively.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. 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.

[2]. 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.

Background

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.

Chemical Properties

Cas No. 864070-44-0 SDF
Synonyms BI 10773
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
Canonical SMILES C1COCC1OC2=CC=C(C=C2)CC3=C(C=CC(=C3)C4C(C(C(C(O4)CO)O)O)O)Cl
Formula C23H27ClO7 M.Wt 450.91
Solubility ≥ 20.75mg/mL in DMSO, ≥ 7.06 mg/mL in EtOH with ultrasonic Storage Store at RT
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 2.2177 mL 11.0887 mL 22.1774 mL
5 mM 0.4435 mL 2.2177 mL 4.4355 mL
10 mM 0.2218 mL 1.1089 mL 2.2177 mL
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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. )

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Average Rating: 5 ★★★★★ (Based on Reviews and 30 reference(s) in Google Scholar.)

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