Art. -Nr.: HY-17604

Bexagliflozin

(Synonyms: EGT1442; EGT0001442; THR-1442)

1 Cited Publications

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Based on 1 publication(s) in Google Scholar

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 HbA_1c 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.

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Reinheit: 99.31%
CAS. Nr.: 1118567-05-7
Formel: C₂₄H₂₉ClO₇
Molecular Weight:464.94

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Bexagliflozin Chemical Structure

CAS. Nr.: 1118567-05-7

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (1)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

hSGLT2

2 nM (IC₅₀)

hSGLT1

5.6 μM (IC₅₀)

Alle SGLT Isoform-spezifische Produkte anzeigen :

SGLT1
SGLT2

Cellular Effect

Cell Line	Type	Value	Description	References
COS-7	IC₅₀	2.3 nM Compound: 29	Inhibition of human SGLT2 expressed in african green monkey COS7 cells assessed as inhibition of [14C]-methyl-alpha-D-glucopyranoside uptake after 2 hrs by scintillation counting in presence of 25 % human plasma Inhibition of human SGLT2 expressed in african green monkey COS7 cells assessed as inhibition of [14C]-methyl-alpha-D-glucopyranoside uptake after 2 hrs by scintillation counting in presence of 25 % human plasma	[PMID: 21737266]
HEK293	IC₅₀	5600 nM Compound: 29	Inhibition of human SGLT1 expressed in human 293 cells assessed as inhibition of [14C]-methyl-alpha-D-glucopyranoside uptake after 1.5 hrs by scintillation counting in presence of 25 % human plasma Inhibition of human SGLT1 expressed in human 293 cells assessed as inhibition of [14C]-methyl-alpha-D-glucopyranoside uptake after 1.5 hrs by scintillation counting in presence of 25 % human plasma	[PMID: 21737266]

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 AUC_0-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

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 1118567-05-7
Appearance Solid
Molecular Weight 464.94
Formel C₂₄H₂₉ClO₇
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
Synonyms

EGT1442; EGT0001442; THR-1442
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (1)

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Biochem Pharmacol

Canagliflozin exerts anti-inflammatory effects by inhibiting intracellular glucose metabolism and promoting autophagy in immune cells. [Abstract]

2018 Jun:152:45-59. PMID: 29551587

Lösungsmittel & Löslichkeit

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.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.1508 mL

10.7541 mL

21.5082 mL

5 mM

0.4302 mL

2.1508 mL

4.3016 mL

10 mM

0.2151 mL

1.0754 mL

2.1508 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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.

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

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

This protocol yields a clear solution of ≥ 3 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 (30.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Zhang W, et al. EGT1442, a potent and selective SGLT2 inhibitor, attenuates blood glucose and HbA(1c) levels in db/db mice and prolongs the survival of stroke-prone rats. Pharmacol Res. 2011;63(4):284-293. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Bexagliflozin

1 Cited Publications

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Bexagliflozin

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Publications Citing Use of MedChemExpress (MCE) Bexagliflozin

Alle SGLT Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Bexagliflozin

Membrane Transporter/Ion Channel Compound Library

FDA-Approved Drug Library

Drug Repurposing Compound Library

Anti-diabetic Compound Library

Anti-Cardiovascular Disease Compound Library

Orally Active Compound Library

FDA Approved & Pharmacopeial Drug Library

Anti-Cancer Metabolism Compound Library

Anti-Obesity Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

FDA-Approved Drug Library Mini

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Animal Drug Library

Publications Citing Use of MedChemExpress (MCE) Bexagliflozin

Alle SGLT Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Bexagliflozin Related Classifications

HY-17604 Related Classifications