For research use only. Not for therapeutic Use.
CVN424 is an orally active and selective GPR6 inverse agonist with a Ki of 9.4 nM and an EC50 of 38 nM. CVN424 is brain-penetrant and has the potential for Parkinson disease research[1][2].
CVN424 (Compound 6i) has 265 fold and 68 fold selectivities over GPR3 and GPR12[1].
| Catalog Number | I044556 |
| CAS Number | 2254706-21-1 |
| Synonyms | 1-[2-[4-(2,4-difluorophenoxy)piperidin-1-yl]-3-[[(3R)-oxolan-3-yl]amino]-7,8-dihydro-5H-pyrido[3,4-b]pyrazin-6-yl]ethanone |
| Molecular Formula | C24H29F2N5O3 |
| Purity | ≥95% |
| InChI | InChI=1S/C24H29F2N5O3/c1-15(32)31-10-6-20-21(13-31)28-23(27-17-7-11-33-14-17)24(29-20)30-8-4-18(5-9-30)34-22-3-2-16(25)12-19(22)26/h2-3,12,17-18H,4-11,13-14H2,1H3,(H,27,28)/t17-/m1/s1 |
| InChIKey | HSWVJQBEXRKOBZ-QGZVFWFLSA-N |
| SMILES | CC(=O)N1CCC2=C(C1)N=C(C(=N2)N3CCC(CC3)OC4=C(C=C(C=C4)F)F)NC5CCOC5 |
| Reference | [1]. Huikai Sun, et al. First-Time Disclosure of CVN424, a Potent and Selective GPR6 Inverse Agonist for the Treatment of Parkinson’s Disease: Discovery, Pharmacological Validation, and Identification of a Clinical Candidate. J Med Chem. 2021 Apr 16. [2]. Nicola L Brice, et al. Development of CVN424: A Selective and Novel GPR6 Inverse Agonist Effective in Models of Parkinson Disease. J Pharmacol Exp Ther. 2021 Jun;377(3):407-416. |
