| Identification | Back Directory | [Name]
Ethanone, 1-[2-[4-(2,4-difluorophenoxy)-1-piperidinyl]-7,8-dihydro-3-[[(3R)-tetrahydro-3-furanyl]amino]pyrido[3,4-b]pyrazin-6(5H)-yl]- | [CAS]
2254706-21-1 | [Synonyms]
penetrant,CVN 424,GPR6,inhibit,orally,CVN424,brain,Inhibitor,Parkinson,CVN-424,disease
Ethanone, 1-[2-[4-(2,4-difluorophenoxy)-1-piperidinyl]-7,8-dihydro-3-[[(3R)-tetrahydro-3-furanyl]ami
Ethanone, 1-[2-[4-(2,4-difluorophenoxy)-1-piperidinyl]-7,8-dihydro-3-[[(3R)-tetrahydro-3-furanyl]amino]pyrido[3,4-b]pyrazin-6(5H)-yl]- | [Molecular Formula]
C24H29F2N5O3 | [MDL Number]
MFCD34471695 | [MOL File]
2254706-21-1.mol | [Molecular Weight]
473.52 |
| Chemical Properties | Back Directory | [Boiling point ]
686.6±55.0 °C(Predicted) | [density ]
1.351±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 62.5 mg/mL (131.99 mM; Need ultrasonic) | [form ]
Solid | [pka]
6.72±0.20(Predicted) | [color ]
Light yellow to green yellow |
| Hazard Information | Back Directory | [Uses]
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]. | [References]
[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. DOI:10.1021/acs.jmedchem.0c02081
[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. DOI:10.1124/jpet.120.000438 |
|
|