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PF-4800567

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Chemical Structure| 1188296-52-7 同义名 : -
CAS号 : 1188296-52-7
货号 : A558311
分子式 : C17H18ClN5O2
纯度 : 99%+
分子量 : 359.81
MDL号 : MFCD22123245
存储条件：

粉末 Keep in dark place,Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 60 mg/mL(166.75 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • CK1

    casein kinase 1 epsilon, IC50:32 nM

    casein kinase 1 delta, IC50:711 nM
描述 Casein kinase 1 ε (CK1ε) and casein kinase 1 δ (CK1δ) are closely related Ser-Thr protein kinases that serve as key clock regulators as demonstrated by mammalian mutations in each that dramatically alter the circadian period. PF-4800567 is a novel and potent inhibitor of CK1ε (IC50 = 32 nM) with greater than 20-fold selectivity over CK1δ (IC50 = 711 nM). PF-4800567 effectively blocked nuclear translocation mediated by CK1ε down to 0.01 μM. Further, PF-4800567 could completely block the enhanced PER2 degradation. These data show that each of the modulatory roles that CK1ε has on the PER proteins can be potently inhibited by PF-4800567. In addition, PF-4800567 had minor effect on the circadian clock at concentrations up to 30 nM. In C57BL/6J mice, PF-4800567 (100 mg/kg, s.c.) was rapidly absorpted and distributed in plasma and brain of mice. The brain-to-plasma ratios was constant throughout the 24-h time course with an average value of 2.1. F-4800567 (100 mg/kg; dosed daily for 3days) delayed the active period by 0.5 h[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.78mL

0.56mL

0.28mL

13.90mL

2.78mL

1.39mL

27.79mL

5.56mL

2.78mL
参考文献

[1]Walton KM, et al. Selective inhibition of casein kinase 1 epsilon minimally alters circadian clock period. J Pharmacol Exp Ther. 2009 Aug;330(2):430-9