KGA-2727 CAS号: 666842-36-0分子式: C26H40N4O8分子量: 536.62描述纯度储存/保存方法别名可溶性/溶解性In vitro(体外研究)In vivo(体内研究)
产品描述 | |
描述 |
KGA-2727 is a potent, selective, high-affinity inhibitor of sodium glucose cotransporter 1 (SGLT1) with Ki of 97.4 nM and 43.5 nM for human SGLT1 and rat SGLT1, respectively. The selectivity ratios (Ki for SGLT2/Ki for SGLT1) of KGA-2727 are 140 (human) and 390 (rat). KGA-2727 exhibits antidiabetic efficacy in rodent models.
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纯度 |
98%
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储存/保存方法 |
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
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基本信息 | |
别名 |
KGA2727
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可溶性/溶解性 |
DMSO :100 mg/mL (186.35 mM)
Water :100 mg/mL (186.35 mM) Ethanol :45 mg/mL (83.86 mM) |
生物活性 | |
In vitro(体外研究) |
KGA-2727 inhibits SGLT1 potently and highly selectively in an in vitro assay using cells transiently expressing recombinant SGLTs.
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In vivo(体内研究) |
In a small intestine closed loop JPorption test with normal rats, KGA-2727 inhibits the JPorption of glucose but not that of fructose. In the oral glucose tolerance test with streptozotocininduced diabetic rats, KGA-2727 attenuats the elevation of plasma glucose after glucose loading, indicating that KGA-2727 improves postprandial hyperglycemia. 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. In addition, the chronic treatment with KGA-2727 increases the level of glucagon-like peptide-1 in the portal vein.
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分子结构图