ChemicalBook--->CAS DataBase List--->666842-36-0

666842-36-0

666842-36-0 Structure

666842-36-0 Structure
IdentificationBack Directory
[Name]

KGA2727
[CAS]

666842-36-0
[Synonyms]

KGA2727
Propanamide, 3-[[3-[4-[[3-(β-D-glucopyranosyloxy)-5-(1-methylethyl)-1H-pyrazol-4-yl]methyl]-3-methylphenoxy]propyl]amino]-
[Molecular Formula]

C26H40N4O8
[MOL File]

666842-36-0.mol
[Molecular Weight]

536.63
Chemical PropertiesBack Directory
[Boiling point ]

839.6±65.0 °C(Predicted)
[density ]

1.308±0.06 g/cm3(Predicted)
[form ]

Solid
[pka]

12.65±0.70(Predicted)
[color ]

White to yellow
Hazard InformationBack Directory
[Uses]

KGA-2727 is a first selective, high-affinity and orally active SGLT1 inhibitor with Kis of 97.4 nM and 43.5 nM for human and rat SGLT1, respectively. The selectivity ratios (Ki for SGLT2/Ki for SGLT1) of KGA-2727 are 140 (human) and 390 (rat). KGA-2727 has antidiabetic efficacy[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. DOI:10.1124/jpet.112.193045
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