| Bioactivity | 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]. | ||||||||||||
| Target | Ki: 9.4 nM (GPR6)EC50: 38 nM (GPR6) | ||||||||||||
| Invitro | CVN424 (Compound 6i) has 265 fold and 68 fold selectivities over GPR3 and GPR12[1]. | ||||||||||||
| Name | CVN424 | ||||||||||||
| CAS | 2254706-21-1 | ||||||||||||
| Formula | C24H29F2N5O3 | ||||||||||||
| Molar Mass | 473.52 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| 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. |
CVN424
CAS: 2254706-21-1 F: C24H29F2N5O3 W: 473.52
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-
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