PF-670462, ≥98%(HPLC)
Product Name： PF-670462
CAS号:950912-80-8
分子式:C19H20FN5·2HCl
分子量:410.32
贮存： 储存温度-20°C
可溶性： DMSO 100 mM Water
生化和生理学机理：
PF-670462, a selective CK1 ε/δ inhibitor, causes a significant phase delay in animal models of circadian rhythm; it remains unclear whether one of the kinases has a predominant role in regulating the circadian clock. PF-670462 has been proved to be both a potent (IC50 = 7.7 ± 2.2 nM) and selective (>30-fold with respect to 42 additional kinases) inhibitor of CK1ε in isolated enzyme preparations; in transfected whole cell assays, it caused a concentration-related redistribution of nuclear versus cytosolic PER. When tested in free-running animals, 50 mg/kg s.c. PF-670462 produced robust phase delays when dosed at circadian time (CT)9 (-1.97 ± 0.17 h). PF-670462 attenuates methamphetamine-stimulated locomotion in vivo.
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