AS 1269574 是口服有效的GPR119激动剂，在表达人 GPR119 的 HEK293 细胞中EC50为 2.5 μM。它激活 TRPA1 阳离子通道，刺激胰高血糖素样肽-1分泌。它仅在高糖条件下特异性诱导胰腺 β 细胞分泌葡萄糖依赖性胰岛素。它在 2 型糖尿病的研究中具有价值。

AS 1269574 is a potent, orally available GPR119 agonist. AS1269574 has the potential for the research of type 2 diabetes.

AS1269574 had an EC(50) value of 2.5μM in HEK293 cells transiently expressing human GPR119 and enhanced insulin secretion in the mouse pancreatic β-cell line MIN-6 only under high-glucose (16.8mM) conditions.?This contrasted with the action of the sulfonylurea glibenclamide, which also induced insulin secretion under low-glucose conditions (2.8mM)[1].

In in vivo studies, a single administration of AS1269574 to normal mice reduced blood glucose levels after oral glucose loading based on the observed insulin secretion profiles.?Significantly, AS1269574 did not affect fed and fasting plasma glucose levels in normal mice.?AS1269574 represents a novel structural class of small molecule, orally administrable GPR119 agonists with GSIS and promising potential for the treatment of type 2 diabetes[1].

330981-72-1

C13H14BrN3O

308.18

AS 1269574

DMSO:250 mg/mL (811.24 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years