Chemical Structure : CVN527
CAS No.:
1799967-04-6
CVN527
(CVN-527)
Catalog No.: 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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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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.
Physicochemical Properties
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M.Wt
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445.51
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Formula
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C23H29F2N5O2
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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1-(2-(4-(2,4-difluorophenoxy)piperidin-1-yl)-3-(isopropylamino)-7,8-dihydropyrido[3,4-b]pyrazin-6(5H)-yl)ethan-1-one
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References
1. Moura-Assis A, et al. Nat Commun. 2026 Jan 13. doi: 10.1038/s41467-025-68056-x.
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