Empagliflozin (BI 10773)SGLT-2 inhibitor for oral treatment of type 2 diabetes CAS# 864070-44-0 |
- GPR40 Activator 1
Catalog No.:BCC4125
CAS No.:1309435-60-6
- TUG-770
Catalog No.:BCC2018
CAS No.:1402601-82-4
- Imeglimin hydrochloride
Catalog No.:BCC4085
CAS No.:775351-61-6
- Imeglimin
Catalog No.:BCC4221
CAS No.:775351-65-0
- Teneligliptin hydrobromide
Catalog No.:BCC1992
CAS No.:906093-29-6
- Chlorpropamide
Catalog No.:BCC4647
CAS No.:94-20-2
Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
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. |
Description | Empagliflozin (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. | |||||
Targets | SGLT-2 | |||||
IC50 | 3.1 nM |
Empagliflozin (BI 10773) Dilution Calculator
Empagliflozin (BI 10773) Molarity Calculator
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. |
Calcutta University
University of Minnesota
University of Maryland School of Medicine
University of Illinois at Chicago
The Ohio State University
University of Zurich
Harvard University
Colorado State University
Auburn University
Yale University
Worcester Polytechnic Institute
Washington State University
Stanford University
University of Leipzig
Universidade da Beira Interior
The Institute of Cancer Research
Heidelberg University
University of Amsterdam
University of Auckland
TsingHua University
The University of Michigan
Miami University
DRURY University
Jilin University
Fudan University
Wuhan University
Sun Yat-sen University
Universite de Paris
Deemed University
Auckland University
The University of Tokyo
Korea University
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.
- ZIP
Catalog No.:BCC4003
CAS No.:863987-12-6
- Mc-MMAE
Catalog No.:BCC5201
CAS No.:863971-24-8
- Methoxy-X04
Catalog No.:BCC6331
CAS No.:863918-78-9
- Fluconazole
Catalog No.:BCC4905
CAS No.:86386-73-4
- Methyl diacetoxy-6-gingerdiol
Catalog No.:BCN3268
CAS No.:863780-90-9
- Diacetoxy-4-gingerdiol
Catalog No.:BCN3337
CAS No.:863780-88-5
- Ganoderic acid X
Catalog No.:BCN7971
CAS No.:86377-53-9
- Ganoderic acid Y
Catalog No.:BCN2439
CAS No.:86377-52-8
- 5,8-Epidioxyergosta-6,9(11),22-trien-3-ol
Catalog No.:BCN1327
CAS No.:86363-50-0
- 6-Epiharpagide
Catalog No.:BCN4563
CAS No.:86362-16-5
- Gnetol
Catalog No.:BCN3382
CAS No.:86361-55-9
- Cebranopadol
Catalog No.:BCC1467
CAS No.:863513-91-1
- GSK429286A
Catalog No.:BCC2532
CAS No.:864082-47-3
- AMG 548
Catalog No.:BCC6084
CAS No.:864249-60-5
- C 021 dihydrochloride
Catalog No.:BCC6047
CAS No.:864289-85-0
- BNTX maleate
Catalog No.:BCC6838
CAS No.:864461-31-4
- Sanggenone K
Catalog No.:BCN3373
CAS No.:86450-77-3
- Sanggenone H
Catalog No.:BCN2946
CAS No.:86450-80-8
- Nigrolineaxanthone V
Catalog No.:BCN4411
CAS No.:864516-31-4
- Sequosempervirin B
Catalog No.:BCN4777
CAS No.:864719-17-5
- Sequosempervirin D
Catalog No.:BCN4562
CAS No.:864719-19-7
- SB 699551
Catalog No.:BCC7594
CAS No.:864741-95-7
- TC-MCH 7c
Catalog No.:BCC6149
CAS No.:864756-35-4
- Gnetucleistol B
Catalog No.:BCN3585
CAS No.:864763-60-0
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.