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Details

Stereochemistry ABSOLUTE
Molecular Formula C24H29ClO7
Molecular Weight 464.936
Optical Activity UNSPECIFIED
Defined Stereocenters 5 / 5
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of BEXAGLIFLOZIN

SMILES

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

InChI

InChIKey=BTCRKOKVYTVOLU-SJSRKZJXSA-N
InChI=1S/C24H29ClO7/c25-19-8-3-15(24-23(29)22(28)21(27)20(13-26)32-24)12-16(19)11-14-1-4-17(5-2-14)30-9-10-31-18-6-7-18/h1-5,8,12,18,20-24,26-29H,6-7,9-11,13H2/t20-,21-,22+,23-,24+/m1/s1

HIDE SMILES / InChI

Molecular Formula C24H29ClO7
Molecular Weight 464.936
Charge 0
Count
MOL RATIO 1 MOL RATIO (average)
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 5 / 5
E/Z Centers 0
Optical Activity UNSPECIFIED

Description

Bexagliflozin, also known as EGT1442, is a potent and selective SGLT2 inhibitor. Bexagliflozin is under investigation for the treatment of Type 2 Diabetes Mellitus. Bexagliflozin has been investigated for the treatment of Diabetes Mellitus and Type2 Diabetes Mellitus. Clinical studies have established that bexagliflozin significantly reduces blood glucose and glycated hemoglobin in subjects with diabetes. Treatment with bexagliflozin also induces weight loss and a reduction in systolic and diastolic blood pressure.

Originator

Approval Year

Targets

Primary TargetPharmacologyConditionPotency
2.0 nM [IC50]

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Unknown

Cmax

ValueDoseCo-administeredAnalytePopulation
692 ng × eq/g
50 mg single, oral
BEXAGLIFLOZIN plasma
Homo sapiens

AUC

ValueDoseCo-administeredAnalytePopulation
2604 ng × eq × h/g
50 mg single, oral
BEXAGLIFLOZIN plasma
Homo sapiens

T1/2

ValueDoseCo-administeredAnalytePopulation
5.6 h
50 mg single, oral
BEXAGLIFLOZIN plasma
Homo sapiens

Overview

Drug as victim

PubMed

Sample Use Guides

In Vivo Use Guide
Each subject with Type 2 Diabetes Mellitus will receive a bexagliflozin tablet, 20 mg, once daily for the duration of the study.
Route of Administration: Oral
In Vitro Use Guide
Bexagliflozin (EGT1442) inhibited SGLT1 and SGLT2-mediated sodium-dependent AMG uptake in a dose-dependent manner. EGT1442 exhibited an IC50 of 2 nM with a 2435-fold selectivity ratio against SGLT2 compared to SGLT1.
Substance Class Chemical
Record UNII
EY00JF42FV
Record Status Validated (UNII)
Record Version