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- 保存条件：
Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.
- 库存：
货期：1-2天
- 供应商：
MedChemExpress LLC
- CAS号：
832714-46-2
- 规格：
10 mM * 1 mL/1 mg/5 mg/10 mg/25 mg/50 mg
| 规格： | 10 mM * 1 mL | 产品价格： | ￥1366.0 |
|---|---|---|---|
| 规格： | 1 mg | 产品价格： | ￥623.0 |
| 规格： | 5 mg | 产品价格： | ￥1300.0 |
| 规格： | 10 mg | 产品价格： | ￥2000.0 |
| 规格： | 25 mg | 产品价格： | ￥3938.0 |
| 规格： | 50 mg | 产品价格： | ￥5900.0 |
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APD668
CAS No. : 832714-46-2
MCE 国际站：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 (Ki=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 (tmax≤2 h) in mice, rats, and monkeys, but slower in dogs (tmax=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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文献和实验NSMB：徐华强 / 谢欣 / 蒋轶发现孤儿受体 GPR119 内源性配体的分子机制
119。研究发现，在不加任何外源配体的情况下，GPR119 即能结合细胞膜中的溶血磷脂酰胆碱（lysophosphatidylcholines，LPC）并被其激活，完美解释了一些受体的所谓「自激活」现象其实是由未知内源配体导致。研究还解析了 GPR119 与临床阶段小分子候选药物 APD668 复合物的冷冻电镜结构，并阐明了受体偶联下游 Gs 信号蛋白的分子机制。 为了研究 GPR119 的结构，研究人员从昆虫细胞中表达纯化了人源 GPR119 受体和 Gs 蛋白三聚体的复合物样品，并在未加入小分子配体
三句话读懂一篇 CNS：代糖也有害！影响肠道菌群，改变血糖水平；瘫痪小鼠成功恢复行走
论文 Structural identification of lysophosphatidylcholines as activating ligands for orphan receptor GPR119。 该研究首次报道孤儿受体 GPR119 偏好性结合 LPC 的分子机制，GPR119 与内源性配体 LPC 以及临床候选小分子药物 APD668 的结构，为靶向 GPR119 的代谢性疾病药物开发提供了重要的结构基础！ 图 8：来源 Natural Structural & Molecular
785.2 H2 O [ml] 948.35 895 840.65 784.6 727.15 668.2 607.55 545.7 %(w/w) 9.379 17.988 25.940 33.350 40.295 46.846 53.070 58.998 H2 O %(w/w) 90.621 82.012 74.060 66.650 59.705 53.154 46.930 41.002 p (g
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