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Empagliflozin [864070-44-0]

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Cat# HY-15409-1g

Size : 1g

Brand : MedChemExpress

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Empagliflozin (BI 107730 is a selective sodium glucose cotransporter-2 (SGLT-2) inhibitor with an IC₅₀ of 3.1 nM for human SGLT-2.

For research use only. We do not sell to patients.

Empagliflozin Chemical Structure

CAS No. : 864070-44-0

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	In-stock	Estimated Time of Arrival: December 31
500 mg	In-stock	Estimated Time of Arrival: December 31
1 g	In-stock	Estimated Time of Arrival: December 31
5 g	In-stock	Estimated Time of Arrival: December 31
10 g	In-stock	Estimated Time of Arrival: December 31
50 g	Get quote

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Based on 67 publication(s) in Google Scholar

Other Forms of Empagliflozin:

Empagliflozin-d₄ Get quote
Empagliflozin (Standard) Get quote

: Empagliflozin purchased from MedChemExpress. Usage Cited in: Biochem Pharmacol. 2018 Jun;152:45-59. [Abstract]; Effects of BMS-512148 and Empagliflozin on p62 expression in LPS-untreated and LPS-treated RAW264.7 cells.

: Empagliflozin purchased from MedChemExpress. Usage Cited in: JACC Basic Transl Sci. 2017 Aug;2(3):347-354.; Improved In Vivo Cardiac Function in Empagliflozin-Treated Mice With Heart Failure Is PreservedEx Vivo. Hearts from vehicle- and Empa-treated mice with HF are perfused ex vivo to measure cardiac function. Cardiac output (A) and cardiac work (B) are measured using ex vivo perfused working hearts.

Description

Empagliflozin (BI 107730 is a selective sodium glucose cotransporter-2 (SGLT-2) inhibitor with an IC₅₀ of 3.1 nM for human SGLT-2^[1].

IC₅₀ & Target

IC50: 3.1 nM (SGLT-2), 1.1 μM (SGLT-5), 2 μM (SGLT-6), 8.3 μM (SGLT-1), 11 μM (SGLT-4)^[1]

In Vitro

Empagliflozin is a potent and competitive SGLT-2 inhibitor with an excellent selectivity profile and the highest selectivity window of the tested SGLT-2 inhibitors over hSGLT-1. Empagliflozin inhibits the uptake of [¹⁴C]-alpha-methyl glucopyranoside (AMG) via hSGLT-2 in a dose-dependent manner with an IC₅₀ of 3.1 nM, but is less potent for other SGLTs (IC₅₀ range: 1100-11000 nM). [³H]-Empagliflozin displays a high affinity for SGLT-2 with a mean K_d of 57±37 nM in the absence of glucose in kinetic binding experiments^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Glucose intolerance is significantly improved after 8 days of Empagliflozin treatment at either dose (3mg/kg Empagliflozin 3058±180 vs 10mg/kg Empagliflozin 3090±219). Therefore, acute treatment with Empagliflozin has a beneficial effect on hyperglycemia and glucose intolerance. Since there are no significant differences in blood glucose homeostasis with the two different doses of Empagliflozin, and random blood glucose levels of T1DM mice are significantly improved by 3mg/kg of Empagliflozin, the effect of the lower dose of Empagliflozin (3mg/kg) is investigated on preserving β-cell mass and function^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

Molecular Weight

450.91

Formula

C₂₃H₂₇ClO₇

CAS No.

864070-44-0

Appearance

Solid

Color

White to off-white

SMILES

ClC(C=CC([C@@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O)=C2)=C2CC(C=C3)=CC=C3O[C@H]4CCOC4

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 250 mg/mL (554.43 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 0.11 mg/mL (0.24 mM; Need ultrasonic and warming)

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% Saline
Solubility: ≥ 2.87 mg/mL (6.36 mM); Clear solution
Protocol 2

Add each solvent one by one: 5% DMSO 95% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.87 mg/mL (6.36 mM); Clear solution
Protocol 3

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (4.61 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 4

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (4.61 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 5

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (4.61 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 0.5% HPMC in Water
Solubility: 5 mg/mL (11.09 mM); Suspension solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.90%

Select Batch:

SDS (393 KB)

COA (249 KB) LCMS (132 KB) Elemental Analysis Report (106 KB)

Handling Instructions (2659 KB)

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 Jan;14(1):83-90. [Content Brief]

[2]. Cheng ST, et al. The Effects of Empagliflozin, an SGLT2 Inhibitor, on Pancreatic β-Cell Mass and Glucose Homeostasis in Type 1 Diabetes. PLoS One. 2016 Jan 25;11(1):e0147391. [Content Brief]

[3]. Nikole J.ByrneBSc, et al. Empagliflozin Prevents Worsening of Cardiac Function in an Experimental Model of Pressure Overload-Induced Heart Failure. JACC Basic Transl Sci. 2017 Aug;2(4):347-354.

[4]. Sakaeda T, et al. Susceptibility to serious skin and subcutaneous tissue disorders and skin tissue distribution of sodium-dependent glucose co-transporter type 2 (SGLT2) inhibitors. Int J Med Sci. 2018 Jun 13;15(9):937-943. [Content Brief]

Animal Administration ^[2]	Mice^[2] Male C57BL/6J mice (10 weeks of age) are used. Empagliflozin is dissolved in hydroxy ethyl cellulose (HEC) and administered to mice in the experimental group (3 or 10 mg/kg) by oral gavage once daily for 8 days, whereas the vehicle group is given same volume of HEC alone. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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 Jan;14(1):83-90. [Content Brief] [2]. Cheng ST, et al. The Effects of Empagliflozin, an SGLT2 Inhibitor, on Pancreatic β-Cell Mass and Glucose Homeostasis in Type 1 Diabetes. PLoS One. 2016 Jan 25;11(1):e0147391. [Content Brief] [3]. Nikole J.ByrneBSc, et al. Empagliflozin Prevents Worsening of Cardiac Function in an Experimental Model of Pressure Overload-Induced Heart Failure. JACC Basic Transl Sci. 2017 Aug;2(4):347-354. [4]. Sakaeda T, et al. Susceptibility to serious skin and subcutaneous tissue disorders and skin tissue distribution of sodium-dependent glucose co-transporter type 2 (SGLT2) inhibitors. Int J Med Sci. 2018 Jun 13;15(9):937-943. [Content Brief]

Animal Administration
^[2]

Mice^[2]
Male C57BL/6J mice (10 weeks of age) are used. Empagliflozin is dissolved in hydroxy ethyl cellulose (HEC) and administered to mice in the experimental group (3 or 10 mg/kg) by oral gavage once daily for 8 days, whereas the vehicle group is given same volume of HEC alone.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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 Jan;14(1):83-90. [Content Brief]

[2]. Cheng ST, et al. The Effects of Empagliflozin, an SGLT2 Inhibitor, on Pancreatic β-Cell Mass and Glucose Homeostasis in Type 1 Diabetes. PLoS One. 2016 Jan 25;11(1):e0147391. [Content Brief]

[3]. Nikole J.ByrneBSc, et al. Empagliflozin Prevents Worsening of Cardiac Function in an Experimental Model of Pressure Overload-Induced Heart Failure. JACC Basic Transl Sci. 2017 Aug;2(4):347-354.

[4]. Sakaeda T, et al. Susceptibility to serious skin and subcutaneous tissue disorders and skin tissue distribution of sodium-dependent glucose co-transporter type 2 (SGLT2) inhibitors. Int J Med Sci. 2018 Jun 13;15(9):937-943. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.2177 mL	11.0887 mL	22.1774 mL	55.4434 mL
	5 mM	0.4435 mL	2.2177 mL	4.4355 mL	11.0887 mL
	10 mM	0.2218 mL	1.1089 mL	2.2177 mL	5.5443 mL
	15 mM	0.1478 mL	0.7392 mL	1.4785 mL	3.6962 mL
	20 mM	0.1109 mL	0.5544 mL	1.1089 mL	2.7722 mL
	25 mM	0.0887 mL	0.4435 mL	0.8871 mL	2.2177 mL
	30 mM	0.0739 mL	0.3696 mL	0.7392 mL	1.8481 mL
	40 mM	0.0554 mL	0.2772 mL	0.5544 mL	1.3861 mL
	50 mM	0.0444 mL	0.2218 mL	0.4435 mL	1.1089 mL
	60 mM	0.0370 mL	0.1848 mL	0.3696 mL	0.9241 mL
	80 mM	0.0277 mL	0.1386 mL	0.2772 mL	0.6930 mL
	100 mM	0.0222 mL	0.1109 mL	0.2218 mL	0.5544 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Empagliflozin Related Classifications

Membrane Transporter/Ion Channel
SGLT

Help & FAQs

Keywords:

Empagliflozin864070-44-0BI 10773BI10773BI-10773SGLTSodium-dependent glucose cotransportersInhibitorinhibitorinhibit

Empagliflozin [864070-44-0]

Cat# HY-15409-1g

Brand : MedChemExpress

Other Forms of Empagliflozin:

Empagliflozin Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Empagliflozin Related Classifications

Keywords:

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