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CVN527

Chemical Structure : CVN527

CAS No.: 1799967-04-6

CVN527 (CVN-527)

货号: PC-25962Not For Human Use, Lab Use Only.

CVN527 is a potent and selective, brain penetrant GPR6 inverse agonist, fully inhibits GPR6 with EC50 of 39.5 nM and 34 nM for mouse and human GPR6 in functional GPR6 cAMP HTRF cell -based assays.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

CVN527 is a potent and selective, brain penetrant GPR6 inverse agonist, fully inhibits GPR6 with EC50 of 39.5 nM and 34 nM for mouse and human GPR6 in functional GPR6 cAMP HTRF cell -based assays.
CVN527 displaces [H3] -RL338 with a Ki of 4.31 nM for native mouse receptor.
CVN527 has similar activity at human and mouse GPR6.
CVN527 is highly brain penetrant in mice.
CVN527 (100 nM) reduced the firing of low -firing DRNVGAT neurons.
CVN527 significantly prevented weight gain in male mice exposed to a high-fat diet by stimulating brown adipose tissue thermogenesis without affecting appetite.

物理化学性质&存储条件

分子量 445.51
分子式 C23H29F2N5O2
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-(2-(4-(2,4-difluorophenoxy)piperidin-1-yl)-3-(isopropylamino)-7,8-dihydropyrido[3,4-b]pyrazin-6(5H)-yl)ethan-1-one

参考文献

1. Moura-Assis A, et al. Nat Commun. 2026 Jan 13. doi: 10.1038/s41467-025-68056-x.

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