WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 314251
CAS#: 864070-44-0
Description: Empagliflozin, also known as BI10773 (trade name Jardiance), is drug approved for the treatment of type 2 diabetes in adults in 2014. It was developed by Boehringer Ingelheim and Eli Lilly and Company. Empagliflozin is an inhibitor of the sodium glucose co-transporter-2 (SGLT-2), and causes sugar in the blood to be absorbed by the kidneys and eliminated in urine. Empagliflozin is an inhibitor of the sodium glucose co-transporter-2 (SGLT-2), which is found almost exclusively in the proximal tubules of nephronic components in the kidneys. SGLT-2 accounts for about 90 percent of glucose reabsorption into the blood.
MedKoo Cat#: 314251
Name: Empagliflozin
CAS#: 864070-44-0
Chemical Formula: C23H27ClO7
Exact Mass: 450.14453
Molecular Weight: 450.91
Elemental Analysis: C, 61.26; H, 6.04; Cl, 7.86; O, 24.84
Synonym: BI10773; BI-10773; BI 10773; CE0108; CS0940; PB23119; VA10802; AJ93046; Empagliflozin; trade name Jardiance.
IUPAC/Chemical Name: (2S,3R,4R,5S,6R)-2-(4-chloro-3-(4-(((S)-tetrahydrofuran-3-yl)oxy)benzyl)phenyl)-6-(hydroxymethyl)tetrahydro-2H-pyran-3,4,5-triol
InChi Key: OBWASQILIWPZMG-QZMOQZSNSA-N
InChi Code: 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
SMILES Code: O[C@H]1[C@H](C2=CC=C(Cl)C(CC3=CC=C(O[C@@H]4COCC4)C=C3)=C2)O[C@H](CO)[C@@H](O)[C@@H]1O
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO (50mg/mL)
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
The following data is based on the product molecular weight 450.91 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
1: Heise T, Mattheus M, Woerle HJ, Broedl UC, Macha S. Assessing Pharmacokinetic Interactions Between the Sodium Glucose Cotransporter 2 Inhibitor Empagliflozin and Hydrochlorothiazide or Torasemide in Patients With Type 2 Diabetes Mellitus: A Randomized, Open-Label, Crossover Study. Clin Ther. 2015 Jan 27. pii: S0149-2918(14)00879-0. doi: 10.1016/j.clinthera.2014.12.018. [Epub ahead of print] PubMed PMID: 25636696.
2: Nishimura R, Tanaka Y, Koiwai K, Inoue K, Hach T, Salsali A, Lund SS, Broedl UC. Effect of empagliflozin monotherapy on postprandial glucose and 24-hour glucose variability in Japanese patients with type 2 diabetes mellitus: a randomized, double-blind, placebo-controlled, 4-week study. Cardiovasc Diabetol. 2015 Jan 30;14(1):11. [Epub ahead of print] PubMed PMID: 25633683.
3: Lewin A, DeFronzo RA, Patel S, Liu D, Kaste R, Woerle HJ, Broedl UC. Initial Combination of Empagliflozin and Linagliptin in Subjects With Type 2 Diabetes. Diabetes Care. 2015 Jan 29. pii: dc142365. [Epub ahead of print] PubMed PMID: 25633662.
4: Kvapil M. [Empagliflozin: another of silent revolutioners]. Vnitr Lek. 2014 Nov;60(11):924-5. Czech. PubMed PMID: 25612346.
5: Ojima A, Matsui T, Nishino Y, Nakamura N, Yamagishi S. Empagliflozin, an Inhibitor of Sodium-Glucose Cotransporter 2 Exerts Anti-Inflammatory and Antifibrotic Effects on Experimental Diabetic Nephropathy Partly by Suppressing AGEs-Receptor Axis. Horm Metab Res. 2015 Jan 22. [Epub ahead of print] PubMed PMID: 25611208.
6: Rušavý Z. [New SGLT2 inhibitor empagliflozin: modern and safe treatment of diabetes]. Vnitr Lek. 2014 Nov;60(11):926-7, 929-30. Czech. PubMed PMID: 25600037.
7: DeFronzo RA, Lewin A, Patel S, Liu D, Kaste R, Woerle HJ, Broedl UC. Combination of Empagliflozin and Linagliptin as Second-Line Therapy in Subjects With Type 2 Diabetes Inadequately Controlled on Metformin. Diabetes Care. 2015 Jan 12. pii: dc142364. [Epub ahead of print] PubMed PMID: 25583754.
8: Chen LZ, Jungnik A, Mao Y, Philip E, Sharp D, Unseld A, Seman L, Woerle HJ, Macha S. Biotransformation and mass balance of the SGLT2 inhibitor empagliflozin in healthy volunteers. Xenobiotica. 2014 Dec 30:1-10. [Epub ahead of print] PubMed PMID: 25547626.
9: Taub ME, Ludwig-Schwellinger E, Ishiguro N, Kishimoto W, Yu H, Wagner K, Tweedie D. Sex-, Species-, and Tissue-Specific Metabolism of Empagliflozin in Male Mouse Kidney Forms an Unstable Hemiacetal Metabolite (M466/2) That Degrades to 4-Hydroxycrotonaldehyde, a Reactive and Cytotoxic Species. Chem Res Toxicol. 2015 Jan 5. [Epub ahead of print] PubMed PMID: 25489797.
10: Scott LJ. Erratum to: Empagliflozin: A Review of Its Use in Patients with Type 2 Diabetes Mellitus. Drugs. 2015 Jan;75(1):141. doi: 10.1007/s40265-014-0336-z. PubMed PMID: 25428712.
