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APD668

CAS No. : 832714-46-2

MCE 站：APD668

产品活性：APD668 是一种有效的，选择性和具有口服活性的 G 蛋白偶联受体 GPR119 激动剂，对 hGPR119 和 rGPR119 的 EC₅₀ 值分别为 2.7 nM 和 33 nM。APD668 对除 CYP2C9 (K_i=0.1 μM) 以外的五种主要 CYP 亚型均无明显抑制作用。APD668 可用于脂肪性肝炎和糖尿病的研究。

研究领域：GPCR/G Protein  |  Neuronal Signaling  |  Metabolic Enzyme/Protease  |  Membrane Transporter/Ion Channel

作用靶点：GPR119  |  Cytochrome P450  |  Potassium Channel

In Vitro: APD668 increases adenylate cyclase activation in HEK293 cells transfected with human GPR119 in a concentration-dependent manner with an EC₅₀ of 23 nM.
APD668 is highly bound to plasma proteins of male ａnd female cynomolgus monkeys ａnd humans (⩾99%), but is less extensively bound to male (93.0%) ａnd female (96.6%) rats.

In Vivo: APD668 (10-30 mg/kg; p.o. once daily for 8 weeks) significantly reduces blood glucose ａnd glycated hemoglobin (HbA1c) levels, with no desensitization of the acute drug response.
APD668 (1-10 mg/kg; a single p.o.) markedly reduces blood glucose levels during oral glucose tolerance test in a dose-dependent manner in mice.
APD668 (0.08 mg/kg/min; i.v.) shows no effect during euglycemic condition, but significantly stimulates insulin release when blood glucose levels are raised to approximately 300 mg/dl in a hyperglycemic clamp model in the Sprague-Dawley rat.
APD668 (p.o.) exhibits rapid to moderate absorption (t_max≤2 h) in mice, rats, ａnd monkeys, but slower in dogs (t_max=6 h), ａnd moderate to good absolute oral bioavailability (44-79%) in mice, rats, ａnd monkeys, but lower in dogs (22%).

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