1. Membrane Transporter/Ion Channel
  2. SGLT
  3. Bexagliflozin

Bexagliflozin  (Synonyms: EGT1442; EGT0001442; THR-1442)

Cat. No.: HY-17604 Purity: 99.31%
Handling Instructions Technical Support

Bexagliflozin (EGT1442) is an orally active and selective SGLT2 inhibitor with IC50 values of 0.002 μM and 5.6 μM for SGLT2 and SGLT1, respectively. Bexagliflozin selectively inhibits SGLT2-mediated sodium-dependent glucose uptake. Bexagliflozin induces saturable urinary glucose excretion in normal rats and dogs. Bexagliflozin reduces blood glucose and HbA1c levels in db/db mice without affecting body mass or insulin level. Bexagliflozin can be used for the research of type 2 diabetes mellitus, hypertensive stroke.

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

Bexagliflozin

Bexagliflozin Chemical Structure

CAS No. : 1118567-05-7

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
In-stock
Solution
10 mM * 1 mL in DMSO In-stock
Solid
5 mg In-stock
10 mg In-stock
25 mg In-stock
50 mg In-stock
100 mg In-stock
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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1 Publications Citing Use of MCE Bexagliflozin

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Description

Bexagliflozin (EGT1442) is an orally active and selective SGLT2 inhibitor with IC50 values of 0.002 μM and 5.6 μM for SGLT2 and SGLT1, respectively. Bexagliflozin selectively inhibits SGLT2-mediated sodium-dependent glucose uptake. Bexagliflozin induces saturable urinary glucose excretion in normal rats and dogs. Bexagliflozin reduces blood glucose and HbA1c levels in db/db mice without affecting body mass or insulin level. Bexagliflozin can be used for the research of type 2 diabetes mellitus, hypertensive stroke[1].

IC50 & Target[1]

hSGLT2

2 nM (IC50)

hSGLT1

5.6 μM (IC50)

In Vitro

Bexagliflozin (EGT1442) potently and selectively inhibits human SGLT2 with an IC50 of 2 nM and 2435-fold selectivity over human SGLT1 in cell-based AMG uptake assays[1].

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

In Vivo

Bexagliflozin (0.1-10 mg/kg; p.o.; single dose) dose-dependently reduces blood glucose AUC0-t and increases urinary glucose excretion in normal Sprague-Dawley rats, with an ED50 of 0.38 mg/kg for urinary glucose excretion[1].
Bexagliflozin (0.03-3 mg/kg; p.o.; single dose) reduces post-glucose challenge blood glucose and induces dose-dependent urinary glucose excretion in normal beagle dogs, with an ED50 of 0.09 mg/kg for urinary glucose excretion[1].
Bexagliflozin (0.1-3 mg/kg; p.o.; daily; 30 days) dose-dependently reduces non-fasting blood glucose and HbA1c levels, and improves oral glucose tolerance in db/db mice over 30 days of daily oral administration, without affecting plasma insulin or body weight[1].
Bexagliflozin (3.0 mg/kg; p.o.; daily via drinking water; up to 2 months) significantly prolongs median survival by approximately 67% (from 32 to 53 days) in SHRSP rats fed a stroke-promoting high-salt diet[1].

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

Animal Model: C57BL/KsJ-db/db (male, 6-8 weeks old, genetic type 2 diabetes model)[1]
Dosage: 0.1 mg/kg; 0.3 mg/kg; 1 mg/kg; 3 mg/kg
Administration: p.o.; daily; 30 days
Result: Dose-dependently reduced non-fasting blood glucose levels from day 1 to day 28, with significant decreases across all treated groups.
Reduced HbA1c levels by 0.51%, 1.08%, 1.13%, and 1.37% for 0.1, 0.3, 1, and 3 mg/kg doses, respectively.
Significantly improved oral glucose tolerance on day 30, with dose-dependent reductions in blood glucose AUC during glucose challenge.
Caused no changes in plasma insulin levels, body weight, food consumption, water consumption, or urine output.
Caused no significant increase in urinary glucose excretion at 2 or 4 weeks compared to control.
Clinical Trial
Molecular Weight

464.94

Formula

C24H29ClO7

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O[C@H]([C@H]1O)[C@@H](O[C@H](CO)[C@H]1O)C2=CC(CC3=CC=C(OCCOC4CC4)C=C3)=C(Cl)C=C2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (215.08 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1508 mL 10.7541 mL 21.5082 mL
5 mM 0.4302 mL 2.1508 mL 4.3016 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 3 mg/mL (6.45 mM); Clear solution

    This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 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 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 3 mg/mL (6.45 mM); Clear solution

    This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

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
References

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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1508 mL 10.7541 mL 21.5082 mL 53.7704 mL
5 mM 0.4302 mL 2.1508 mL 4.3016 mL 10.7541 mL
10 mM 0.2151 mL 1.0754 mL 2.1508 mL 5.3770 mL
15 mM 0.1434 mL 0.7169 mL 1.4339 mL 3.5847 mL
20 mM 0.1075 mL 0.5377 mL 1.0754 mL 2.6885 mL
25 mM 0.0860 mL 0.4302 mL 0.8603 mL 2.1508 mL
30 mM 0.0717 mL 0.3585 mL 0.7169 mL 1.7923 mL
40 mM 0.0538 mL 0.2689 mL 0.5377 mL 1.3443 mL
50 mM 0.0430 mL 0.2151 mL 0.4302 mL 1.0754 mL
60 mM 0.0358 mL 0.1792 mL 0.3585 mL 0.8962 mL
80 mM 0.0269 mL 0.1344 mL 0.2689 mL 0.6721 mL
100 mM 0.0215 mL 0.1075 mL 0.2151 mL 0.5377 mL
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Bexagliflozin
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