Chemical Structure : CVN527
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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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.
| 分子量 | 445.51 | |
| 分子式 | C23H29F2N5O2 | |
| 外观性状 | Solid | |
| 储存条件 |
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| Solubility |
10 mM in DMSO |
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1. Moura-Assis A, et al. Nat Commun. 2026 Jan 13. doi: 10.1038/s41467-025-68056-x.
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