PW0787
规格
| Cas Number | 2624131-45-7 |
| 规格或纯度 | ≥99% |
| 纯度 | ≥99% |
| 包装 | 100mg 或 50mg 或 10mg 或 5mg 或 25mg |
产品信息
| 品牌 | 阿拉丁 |
| 溶解性 | DMSO : 50 mg/mL (108.60 mM; Need ultrasonic) |
| 过滤标签 | GPR52,GPCR/G Protein |
| 储存温度 | 避光,-80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 生化和生理学机理 | PW0787 是一种强效、选择性、口服活性和脑穿透性 GPR52 激动剂（EC 50 =135 nM）。PW0787 可抑制精神兴奋剂行为。 |
| 英文描述 |
PW0787 is a potent, selective, orally active, and brain-penetrant GPR52 agonist ( EC 50 =135 nM). PW0787 suppresses psychostimulant behavior In Vivo PW0787 (0.3, 1, 3, or 10 mg/kg; IP) displays antipsychotic-like activity by significantly inhibiting amphetamine-induced hyperlocomotor behavior in mice . PW0787 is evaluated in rats after a single dose of 20 mg/kg by oral (PO) or 10 mg/kg by intravenous (IV) administration. PW0787 has excellent plasma exposure after PO (AUC 0-inf = 13,749 ng•h/mL) and IV dosing (AUC 0-inf =9030 ng•h/mL), as well as high maximum serum concentration following PO (C max =3407 ng/mL) and IV administration (C max =6726 ng/mL). Additionally, PW0787 displays good volume of plasma distribution (V ss =1.5 L/kg) and acceptable plasma clearance (CL=1.1 L/h/kg) after 10 mg/kg IV. Excellent oral bioavailability (F) with the value of 76% is observed . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Naïve male C57/BL6 mice weighing between 24 and 31 g Dosage: 0.3, 1, 3, or 10 mg/kg (dissolved in 0.9% saline containing 20% HP-β-CD with a final pH of the solution adjusted to 7.4) Administration: IP Result: Suppressed amphetamine (AMPH)-induced horizontal activity at both 3 mg/kg and 10 mg/kg doses. Form:Solid IC50& Target:EC50: 135 nM (GPR52) |