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950912-80-8

中文名稱 4-[1-環(huán)己基-4-(4-氟苯基)-1H-咪唑-5-基]-2-嘧啶胺鹽酸鹽
英文名稱 4-[1-Cyclohexyl-4-(4-fluorophenyl)-1H-imidazol-5-yl]-2-pyrimidinaminedihydrochloride
CAS 950912-80-8
分子式 C19H20FN5.2HCl
分子量 410
MOL 文件 950912-80-8.mol
更新日期 2024/06/03 14:41:43
950912-80-8 結(jié)構(gòu)式 950912-80-8 結(jié)構(gòu)式

基本信息

中文別名
化合物PF670462
CK1Ε抑制劑(PF-670462)
4-[1-環(huán)己基-4-(4-氟苯基)-1H-咪唑-5-基]-2-嘧啶胺鹽酸鹽
英文別名
CS-318
PF 67046
PF 670462
PF-670462 HCL
PF-670462 2HCl
PF 670462, >=98%
PF670462/ PF-670462
PF670462 dihydrochloride
PF-670462 (hydrochloride)
Casein Kinase I Inhibitor II, PF-670462
所屬類別
生物化工:激動劑抑制劑

物理化學(xué)性質(zhì)

熔點(diǎn)>178°C (dec.)
儲存條件2-8°C
溶解度在水中的溶解度為性2mg/mL,澄清(加熱)
形態(tài)粉末
顏色白色至米色
InChIKeyPSNKGVAXBSAHCH-UHFFFAOYSA-N

安全數(shù)據(jù)

危險性符號(GHS)GHS hazard pictograms
GHS07
警示詞警告
危險性描述H302-H315-H319-H335
WGK Germany3

應(yīng)用領(lǐng)域

用途1
PF 670462 is a potent and selective casein kinase 1蔚 (CK1蔚) 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.

常見問題列表

生物活性
PF-670462是有效的、選擇性CK1ε和CK1δ抑制劑,IC50分別為90 nM和13 nM。
靶點(diǎn)
TargetValue
CK1δ
(Cell-free assay)
13 nM
CK1ε
(Cell-free assay)
90 nM
體外研究

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.

體內(nèi)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.

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