Bexagliflozin diproline
Based on 1 publication(s) in Google Scholar
Bexagliflozin diproline (EGT1442 diproline; EGT0001442 diproline; THR-1442 diproline) 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 diproline selectively inhibits SGLT2-mediated sodium-dependent glucose uptake. Bexagliflozin diproline induces saturable urinary glucose excretion in normal rats and dogs. Bexagliflozin diproline reduces blood glucose and HbA1c levels in db/db mice without affecting body mass or insulin level. Bexagliflozin diproline can be used for the research of type 2 diabetes mellitus, hypertensive stroke.
For research use only. We do not sell to patients.
- CAS No.: 1118567-48-8
- Formula: C34H47ClN2O11
- Molecular Weight:695.20
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
- Protocols
- Purity & Documentation
- References
-
Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Bexagliflozin diproline
More
Biological Activity
Description
IC50 & Target
[1]|
hSGLT2 2 nM (IC50) |
hSGLT1 5.6 μM (IC50) |
In Vitro
In Vivo
Bexagliflozin (0.03-3 mg/kg; p.o.; single dose) diproline 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) diproline 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) diproline 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.
Chemical Information
-
CAS No. 1118567-48-8
-
Molecular Weight 695.20
-
Formula C34H47ClN2O11
-
SMILES
OC([C@@H]1CCCN1)=O.O[C@H]2[C@@H](O[C@@H]([C@H]([C@@H]2O)O)CO)C3=CC(CC4=CC=C(C=C4)OCCOC5CC5)=C(C=C3)Cl.OC([C@@H]6CCCN6)=O
-
Synonyms
EGT1442 diproline; EGT0001442 diproline; THR-1442 diproline
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (1)
-
Journal Impact Factor
-
Most Recent
-
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
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Bexagliflozin diproline Related Classifications
HY-17604A Related Classifications
Powered by Bioz