CVN424 是一种具有口服活性和选择性的 GPR6 反向激动剂，EC50 为 9.4 nM，EC50 为 38 nM。CVN424 可以透过血脑屏障，具有用于帕金森病研究的潜力。
货号:ajcx34658
CAS:2254706-21-1
分子式:C24H29F2N5O3
分子量：473.52
溶解度:DMSO : 62.5 mg/mL (131.99 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

CVN424 is an orally active and selective GPR6 inverse agonist with a EC50 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].

[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.