4-[1-环己基-4-(4-氟苯基)-1H-咪唑-5-基]-2-嘧啶胺盐酸盐 CAS#: 950912-80-8

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4-[1-环己基-4-(4-氟苯基)-1H-咪唑-5-基]-2-嘧啶胺盐酸盐

生物活性靶点体外研究体内研究 用途与合成方法 MSDS 4-[1-环己基-4-(4-氟苯基)-1H-咪唑-5-基]-2-嘧啶胺盐酸盐价格(试剂级) 上下游产品信息

中文名称	4-[1-环己基-4-(4-氟苯基)-1H-咪唑-5-基]-2-嘧啶胺盐酸盐
中文同义词	4-[1-环己基-4-(4-氟苯基)-1H-咪唑-5-基]-2-嘧啶胺盐酸盐;CK1Ε抑制剂(PF-670462);化合物PF670462;PF-670462盐酸盐;4-[1-环己基-4-(4-氟苯基)-1H-咪唑-5-基]-2-嘧啶胺二盐酸盐;PF-670462,酪蛋白激酶1Ε(CK1Ε)和CK1Δ抑制剂
英文名称	4-[1-Cyclohexyl-4-(4-fluorophenyl)-1H-imidazol-5-yl]-2-pyrimidinaminedihydrochloride
英文同义词	PF670462/ PF-670462;4-[1-Cyclohexyl-4-(4-fluorophenyl)-1H-imidazol-5-yl]-2-pyrimidinamine hydrochloride;2-PyriMidinaMine, 4-[1-cyclohexyl-4-(4-fluorophenyl)-1H-iMidazol-5-yl]-, hydrochloride (1:2);PF 67046;4-[1-Cyclohexyl-4-(4-fluorophenyl)-1H-imidazol-5-yl]-2-pyrimidinamine hydrochloride                                       PF670462;4-[3-Cyclohexyl-5-(4-fluoro-phenyl)-3H-imidazol-4-yl]-pyrimidin-2-ylamine dihydrochloride;PF 670462, >=98%;PF 670462
CAS号	950912-80-8
分子式	C19H20FN5.2HCl
分子量	410
EINECS号
相关类别	小分子抑制剂，天然产物;信号转导通路激酶抑制剂;抑制剂;小分子抑制剂;细胞生物学试剂;Inhibitors;Aromatics;Heterocycles;Intermediates & Fine Chemicals;Pharmaceuticals;Protein Kinase Inhibitors and Activators
Mol文件	950912-80-8.mol
结构式

4-[1-环己基-4-(4-氟苯基)-1H-咪唑-5-基]-2-嘧啶胺盐酸盐 性质

4-[1-环己基-4-(4-氟苯基)-1H-咪唑-5-基]-2-嘧啶胺盐酸盐 用途与合成方法

生物活性

PF-670462是有效的、选择性CK1ε和CK1δ抑制剂，IC50分别为90 nM和13 nM。

靶点

体外研究

PF-670462 is a potent and selective inhibitor of CKIε and CKIδ, with IC     ₅₀    s of 7.7 nM and 14 nM, respectively. PF-670462 shows less than 30-fold selevtivity for EGFR and SAPK2A/p38, with IC     ₅₀    s of 150 nM and 190 nM, respectively. PF-670462 also causes a redistribution of the GFP signal to the cytoplasm in a concentration-dependent manner, with an EC     ₅₀    of 290 ± 39 nM in CKIε-transfected COS7 cells. PF-670462 is a potent inhibitor of Wnt/β-catenin signaling, with an IC     ₅₀    of ∼17 nM. PF-670462 (1 μM) is a weak inhibitor of proliferation, and only modestly suppresses the growth of HEK293 and HT1080 cells. PF-670462 (100 nM) strongly inhibits CK1ε and CK1δ, consistent with its effect on Wnt/β-catenin signaling.

体内研究

PF-670462 (50 mg/kg, s.c.) produces robust phase delays, and the activity remains persistent, with no discernible correction in the absence of exogenous zeitgebers in rats. PF-670462 (25, 50, and 100 mg/kg, s.c.) induces dose-dependent phase shift. PF-670462 (50 mg/kg; s.c.) significantly phase delays the rhythmic transcription of Bmal1, Per1, Per2 and Nr1d1 in both liver and pancreas by 4.5 ± 1.3 h and 4.5 ± 1.2 h, respectively, 1 day after administration. In the suprachiasmatic nucleus (SCN), the rhythm of Nr1d1 and Dbp mRNA expression is also delayed by 4.2 and 4 h, respectively.

用途 

PF 670462 is a potent and selective casein kinase(CK1ε) and CK1δ inhibitor. PF 670462 has been shown to inhibit PER protein nuclear translocation causing phase shifts in circadian rhythms. PF 6704 62 attenuates methamphetamine-stimulated locomotion in vivo.

安全信息

MSDS信息

4-[1-环己基-4-(4-氟苯基)-1H-咪唑-5-基]-2-嘧啶胺盐酸盐 价格(试剂级)

4-[1-环己基-4-(4-氟苯基)-1H-咪唑-5-基]-2-嘧啶胺盐酸盐 上下游产品信息