PW0787

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

PW0787 是一种有效、选择性、口服活性、脑渗透性 GPR52 激动剂 (EC50=135 nM)。

PW0787 is a potent, selective, orally active, and brain-penetrant GPR52 agonist (EC50=135 nM).

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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 (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. Animal Model:Na?ve 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.

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Cell Cycle/DNA Damage

GPR

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2624131-45-7

460.433

C23H20F4N4O2

>98% (HPLC)

In Vitro:?DMSO : 50 mg/mL (108.60 mM)

OCCNC(=O)c1cccc2N(CCc12)c1cc(Cc2cc(F)cc(c2)C(F)(F)F)ncn1

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(-20℃)

With Ice Pack

≥ 2 years