PW0787

PW0787 是一种有效的，选择性的，具有口服活性的，可透过血脑屏障的 GPR52 激动剂 (EC50=135 nM)。PW0787 抑制精神刺激行为。

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库存: 现货

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5mg

￥1625.00

1300.00

- +
10mg

￥2725.00

2180.00

- +
25mg

￥5400.00

4320.00

- +
50mg

￥8412.00

6730.00

- +
100mg

￥12287.00

9830.00

- +

已选 0 种 0 瓶

金额: ￥0.00

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货号: ajcx35914
CAS: 2624131-45-7
别名:
分子式: C23H20F4N4O2
分子量: 460.42
纯度: >98%
溶解度: DMSO : 50 mg/mL (108.60 mM; Need ultrasonic)
储存: 4°C, protect from light
库存: 现货

Background

PW0787 is a potent, selective, orally active, and brain-penetrant GPR52 agonist (EC50=135 nM). PW0787 suppresses psychostimulant behavior[1].

PW0787 (0.3, 1, 3, or 10 mg/kg; IP) displays antipsychotic-like activity by significantly inhibiting amphetamine-induced hyperlocomotor behavior in mice[1].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 (AUC0-inf = 13,749 ng?h/mL) and IV dosing (AUC0-inf=9030 ng?h/mL), as well as high maximum serum concentration following PO (Cmax=3407 ng/mL) and IV administration (Cmax=6726 ng/mL). Additionally, PW0787 displays good volume of plasma distribution (Vss=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[1].

[1]. Wang P, et al. Discovery of Potent and Brain-Penetrant GPR52 Agonist that Suppresses Psychostimulant Behavior. J Med Chem. 2020;63(22):13951-13972.