Empagliflozin
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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.


Chemical Structure

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Empagliflozin
CAS# 864070-44-0

Theoretical Analysis

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

Price and Availability

Size Price Availability Quantity
10.0mg USD 90.0 Same day
100.0mg USD 150.0 Same day
500.0mg USD 250.0 Same day
1.0g USD 450.0 Same day
2.0g USD 750.0 Same day
5.0g USD 1250.0 Same day
10.0g USD 1950.0 Same day
20.0g USD 2950.0 Same day
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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

Biological target: Empagliflozin (BI 107730) is a sodium glucose cotransporter-2 (SGLT-2) inhibitor with an IC50 of 3.1 nM.
In vitro activity: The effects of empagliflozin on mitochondrial quality control and autophagy in renal tubular cells in a diabetic environment were examined in vitro. Human renal proximal tubular cells (hRPTCs) were incubated under high-glucose conditions. Improvements in mitochondrial biogenesis and balanced fusion-fission protein expression were noted in hRPTCs after treatment with empagliflozin in high-glucose media. Empagliflozin also increased autophagic activities in renal tubular cells in the high-glucose environment, which was accompanied with mammalian target of rapamycin inhibition. Moreover, reduced mitochondrial reactive oxygen species production and decreased apoptotic and fibrotic protein expression were observed in hRPTCs after treatment with empagliflozin, even in the hyperglycemic circumstance. Importantly, empagliflozin restored AMP-activated protein kinase-α phosphorylation and normalized levels of AMP-to-ATP ratios in hRPTCs subjected to a high-glucose environment, which suggests the way that empagliflozin is involved in mitochondrial quality control. Reference: Am J Physiol Renal Physiol. 2019 Oct 1;317(4):F767-F780. https://journals.physiology.org/doi/full/10.1152/ajprenal.00565.2018?rfr_dat=cr_pub++0pubmed&url_ver=Z39.88-2003&rfr_id=ori%3Arid%3Acrossref.org
In vivo activity: To investigate the effect of empagliflozin on myocardium injury and the potential mechanism in type 2 diabetic KK-Ay mice, thirty diabetic KK-Ay mice were administered empagliflozin (10 mg/kg/day) by oral gavage daily for 8 weeks. Results showed that empagliflozin improved diabetic myocardial structure and function, decreased myocardial oxidative stress and ameliorated myocardial fibrosis. Further study indicated that empagliflozin suppressed oxidative stress and fibrosis through inhibition of the transforming growth factor β/Smad pathway and activation of Nrf2/ARE signaling. Reference: Cardiovasc Diabetol. 2019 Feb 2;18(1):15. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6359811/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 56.67 125.68
DMF 30.0 66.53
Ethanol 30.0 66.53
Ethanol:PBS (pH 7.2) (1:1) 0.5 1.11

Preparing Stock Solutions

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.

Recalculate based on batch purity %
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
Formulation protocol: 1. Lee YH, Kim SH, Kang JM, Heo JH, Kim DJ, Park SH, Sung M, Kim J, Oh J, Yang DH, Lee SH, Lee SY. Empagliflozin attenuates diabetic tubulopathy by improving mitochondrial fragmentation and autophagy. Am J Physiol Renal Physiol. 2019 Oct 1;317(4):F767-F780. doi: 10.1152/ajprenal.00565.2018. Epub 2019 Aug 7. PMID: 31390268. 2. Ng KM, Lau YM, Dhandhania V, Cai ZJ, Lee YK, Lai WH, Tse HF, Siu CW. Empagliflozin Ammeliorates High Glucose Induced-Cardiac Dysfuntion in Human iPSC-Derived Cardiomyocytes. Sci Rep. 2018 Oct 5;8(1):14872. doi: 10.1038/s41598-018-33293-2. PMID: 30291295; PMCID: PMC6173708. 3. Li C, Zhang J, Xue M, Li X, Han F, Liu X, Xu L, Lu Y, Cheng Y, Li T, Yu X, Sun B, Chen L. SGLT2 inhibition with empagliflozin attenuates myocardial oxidative stress and fibrosis in diabetic mice heart. Cardiovasc Diabetol. 2019 Feb 2;18(1):15. doi: 10.1186/s12933-019-0816-2. PMID: 30710997; PMCID: PMC6359811.
In vitro protocol: 1. Lee YH, Kim SH, Kang JM, Heo JH, Kim DJ, Park SH, Sung M, Kim J, Oh J, Yang DH, Lee SH, Lee SY. Empagliflozin attenuates diabetic tubulopathy by improving mitochondrial fragmentation and autophagy. Am J Physiol Renal Physiol. 2019 Oct 1;317(4):F767-F780. doi: 10.1152/ajprenal.00565.2018. Epub 2019 Aug 7. PMID: 31390268. 2. Ng KM, Lau YM, Dhandhania V, Cai ZJ, Lee YK, Lai WH, Tse HF, Siu CW. Empagliflozin Ammeliorates High Glucose Induced-Cardiac Dysfuntion in Human iPSC-Derived Cardiomyocytes. Sci Rep. 2018 Oct 5;8(1):14872. doi: 10.1038/s41598-018-33293-2. PMID: 30291295; PMCID: PMC6173708.
In vivo protocol: 1. Li C, Zhang J, Xue M, Li X, Han F, Liu X, Xu L, Lu Y, Cheng Y, Li T, Yu X, Sun B, Chen L. SGLT2 inhibition with empagliflozin attenuates myocardial oxidative stress and fibrosis in diabetic mice heart. Cardiovasc Diabetol. 2019 Feb 2;18(1):15. doi: 10.1186/s12933-019-0816-2. PMID: 30710997; PMCID: PMC6359811. 2. Lee YH, Kim SH, Kang JM, Heo JH, Kim DJ, Park SH, Sung M, Kim J, Oh J, Yang DH, Lee SH, Lee SY. Empagliflozin attenuates diabetic tubulopathy by improving mitochondrial fragmentation and autophagy. Am J Physiol Renal Physiol. 2019 Oct 1;317(4):F767-F780. doi: 10.1152/ajprenal.00565.2018. Epub 2019 Aug 7. PMID: 31390268.

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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.