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PW0787

Chemical Structure : PW0787

CAS No.: 2624131-45-7

PW0787 (PW 0787, PW-0787)

货号: PC-72127Not For Human Use, Lab Use Only.

PW0787 (PW 0787) is a potent, selective, brain-penetrant GPR52 agonist with EC50 of 135 nM in cAMP assays in HEK293 cells.

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5 mg ¥1280 In stock
10 mg ¥1980 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

PW0787 (PW 0787) is a potent, selective, brain-penetrant GPR52 agonist with EC50 of 135 nM in cAMP assays in HEK293 cells.
PW0787displays no significant binding affinity (IC50>10 uM) against other GPCRs, a broad-panel counter screening (NIMH-PDSP), as well as hERG potassium channel.
PW0787 exhibits a good concentration in the brain at 0.25 h with the value of 1807 ng/g and also exhibits an acceptable brain permeability with a brain/plasma ratio of 0.28. 
PW0787 is an orally bioavailable and brain-penetrant GPR52 agonist with antipsychotic-like activity, which dose-dependently inhibits amphetamine-evoked hyperactivity in mice.

物理化学性质&存储条件

分子量 460.433
分子式 C23H20F4N4O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

1-(6-(3-Fluoro-5-(trifluoromethyl)benzyl)pyrimidin-4-yl)-N-(2-hydroxyethyl)indoline-4-carboxamide

参考文献

1. Pingyuan Wang, et al. J Med Chem. 2020 Nov 25;63(22):13951-13972.

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