| Size | Price | Stock | Qty |
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| 25mg |
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| 100mg |
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Purity: = 99.86%
Empagliflozin (formerly also known as BI1-0773; CE0108; CS0940; PB23119; VA10802; AJ93046; trade name: Jardiance) is a potent and selective SGLT-2 (sodium glucose cotransporter-2) inhibitor with anti-diabetic activity. It shows >300-fold selectivity over SGLT-1, 4, 5, and 6 and inhibits SGLT2 with an IC50 of 3.1 nM. For the treatment of adult patients with type 2 diabetes, the FDA has approved empagliflozin. Blood sugar is absorbed by the kidneys and excreted in urine as a result of empagliflozin's inhibition of the sodium glucose co-transporter-2 (SGLT-2). Nearly 90% of the blood's reabsorption of glucose is made possible by SGLT-2, which is primarily located in the proximal tubules of the kidney's nephronic components.
| Targets |
SGLT-2 ( IC50 = 3.1 nM ); SGLT-5 ( IC50 = 1.1 μM ); SGLT-6 ( IC50 = 2 μM ); SGLT-1 ( IC50 = 8.3 μM ); SGLT-4 ( IC50 = 11 μM )
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| ln Vitro |
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| Enzyme Assay |
This assay for sodium-dependent monosaccharide transport inhibition uses stable cell lines that overexpress hSGLT-1, -2, -4, -5, or -6 or rSGLT-1 or -2. Pre-incubation of cells is conducted for 25 minutes at 37°C in 200 μL uptake buffer (10 mM HEPES, 137 mM NaCl, 5.4 mM KCl, 2.8 mM CaCl2, 1.2 mM MgCl2, 50 μg/ml Gentamycin, 0.1% BSA). Half an hour before the uptake experiment starts, 10 μM Cytochalasin B and the test compound are added at various concentrations. The addition of 0.6 μCi [14C]-labeled monosaccharide, such as [14C]-labeled AMG, glucose, fructose, mannose, or myo-inositol, to 0.1 mM AMG (or the corresponding non-radioactive monosaccharide) initiates the uptake reaction. The cells are incubated at 37°C for 60 minutes (hSGLT-5), 90 minutes (hSGLT-4), or 4 hours (hSGLT-2) before being washed three times with 300 μL PBS and lysed in 0.1 N NaOH for five minutes while being shaken intermittently. After mixing the lysate with 200 μL MicroScint 40 and shaking it for 15 minutes, the radioactivity is measured using the TopCount NXT. Prior to the addition of uptake buffer, cells are pre-incubated in pre-treatment buffer (uptake buffer containing choline chloride instead of NaCl) for 25 minutes in the case of the SGLT-4 and SGLT-5 tests.
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| Cell Assay |
Empagliflozin treatment competitively binds to SGLT-2 over glucose at low doses, as demonstrated by tests conducted on a panel of human cell lines that overexpress SGLT-1, 2, 4, 5, and 6. 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.
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| References |
| Molecular Formula |
C23H27CLO7
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| Molecular Weight |
450.91
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| Exact Mass |
450.14
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| Elemental Analysis |
C, 61.26; H, 6.04; Cl, 7.86; O, 24.84
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| CAS # |
864070-44-0
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| Related CAS # |
Empagliflozin-d4; 2749293-95-4
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| Appearance |
Solid powder
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| SMILES |
C1COC[C@H]1OC2=CC=C(C=C2)CC3=C(C=CC(=C3)[C@H]4[C@@H]([C@H]([C@@H]([C@H](O4)CO)O)O)O)Cl
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| InChi Key |
OBWASQILIWPZMG-QZMOQZSNSA-N
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| 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
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| 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
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| Synonyms |
BI1-0773; CE0108; CS0940; PB23119; VA10802; AJ93046; BI10773; BI-10773; BI 10773; Empagliflozin; trade name: Jardiance
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 5 mg/mL (11.09 mM) in 0.5%HPMC (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
Solubility in Formulation 2: ≥ 2.87 mg/mL (6.36 mM) (saturation unknown) in 5% DMSO + 40% PEG300 + 5% Tween80 + 50% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.87 mg/mL (6.36 mM) (saturation unknown) in 5% DMSO + 95% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: ≥ 2.08 mg/mL (4.61 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 5: ≥ 2.08 mg/mL (4.61 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 6: ≥ 2.08 mg/mL (4.61 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. Solubility in Formulation 7: 15% Captisol: 15 mg/mL |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT05262764 | Active Recruiting |
Drug: JARDIANCE® | Heart Failure | Boehringer Ingelheim | April 1, 2022 | N/A |
| NCT05350202 | Active Recruiting |
Drug: Empagliflozin | Heart Failure | Boehringer Ingelheim | December 15, 2022 | N/A |
| NCT03437330 | Active Recruiting |
Drug: Empagliflozin (Jardiance®) Drug: Insulin Glargine (Lantus®) |
Type2 Diabetes Mellitus | University Hospital Tuebingen | October 27, 2021 | Phase 4 |
| NCT03363464 | Active Recruiting |
Drug: Empagliflozin Drug: DPP-4 inhibitor |
Diabetes Mellitus, Type 2 | Boehringer Ingelheim | October 16, 2017 | N/A |
| NCT03193684 | Active Recruiting |
Drug: Empagliflozin 25 MG Drug: Control |
Hepatic Glucose Metabolism | The University of Texas Health Science Center at San Antonio |
May 20, 2018 | Phase 4 |
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