666842-36-0

666842-36-0 structure

Name: KGA-2727
Chemical Name: KGA-2727
CAS Number: 666842-36-0
Molecular Formula: C₂₆H₄₀N₄O₈
Molecular Weight: 536.626
Catalog: Signaling Pathways Membrane Transporter/Ion Channel SGLT
Create Date: 2020-01-11 18:26:50
Modify Date: 2024-01-09 18:23:18
KGA-2727 is a potent, selective SGLT1 inhibitor with Ki of 97.4 nM, >100-fold selectivity over SGLT2; attenuates the elevation of plasma glucose after glucose loading in streptozotocin-induced diabetic rats, preserves glucose-stimulated insulin secretion and reduces urinary glucose excretion with improved morphological changes of pancreatic islets and renal distal tubules in ZDF rats.

Name	KGA-2727

Description	KGA-2727 is a potent, selective SGLT1 inhibitor with Ki of 97.4 nM, >100-fold selectivity over SGLT2; attenuates the elevation of plasma glucose after glucose loading in streptozotocin-induced diabetic rats, preserves glucose-stimulated insulin secretion and reduces urinary glucose excretion with improved morphological changes of pancreatic islets and renal distal tubules in ZDF rats.
Related Catalog	Research Areas >> Metabolic Disease Signaling Pathways >> Membrane Transporter/Ion Channel >> SGLT
Target	Ki: 97.4 nM (human SGLT1), 43.5 nM (rat SGLT1)[1]
In Vitro	A Dixon plot analysis for KGA-2727 displays good linearity for human SGLT1 and SGLT2. The results of the Dixon plot show that KGA-2727 inhibits these SGLTs in a competitive manner. KGA2727 dose-dependently inhibits Methyl-Dglucopyranoside (AMG) uptake by SGLT1 and SGLT2[1].
In Vivo	In the oral glucose tolerance test with streptozotocin-induced diabetic rats, KGA-2727 attenuates the elevation of plasma glucose after glucose loading, indicating that KGA-2727 improves postprandial hyperglycemia[1]. In Zucker diabetic fatty (ZDF) rats, chronic treatments with KGA-2727 reduces the levels of plasma glucose and glycated hemoglobin. Furthermore, KGA-2727 preserves glucose-stimulated insulin secretion and reduces urinary glucose excretion with improved morphological changes of pancreatic islets and renal distal tubules in ZDF rats[1].
References	[1]. Shibazaki T, et al. KGA-2727, a novel selective inhibitor of a high-affinity sodium glucose cotransporter (SGLT1), exhibits antidiabetic efficacy in rodent models. J Pharmacol Exp Ther. 2012 Aug;342(2):288-96.

Molecular Formula	C₂₆H₄₀N₄O₈
Molecular Weight	536.626
Storage condition	-20°C

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