6-[4-[2-(1-哌啶基)乙氧基]苯基]-3-(4-吡啶基)吡唑并[1,5-A]嘧啶 - CAS:866405-64-3 - CAS号查询_生物试剂_化学试剂_分析试剂

中文名称:	6-[4-[2-(1-哌啶基)乙氧基]苯基]-3-(4-吡啶基)吡唑并[1,5-A]嘧啶
英文名称:	Dorsomorphin
别名:	AMPK 抑制剂 BML-275
CAS No:	866405-64-3	分子式:	C₂₄H₂₅N₅O	分子量:	399.49
CAS No:	866405-64-3
分子式:	C₂₄H₂₅N₅O
分子量:	399.49
MDL:	MFCD08705402

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D70011 6-[4-[2-(1-哌啶基)乙氧基]苯基]-3-(4-吡啶基)吡唑并[1,5-A]嘧啶 ≥98%(HPLC) (psaitong)

相关产品

外观与性状：

白色粉末

包装规格：

5mg 25mg 100mg in glass bottle

溶解性：

溶于DMSO(4MG/ML加热)和乙醇

产品描述：

基本信息

产品编号：D70011
产品名称：Dorsomorphin
CAS:	866405-64-3	储存条件	粉末	2-8℃	四年
分子式：	C24H25N5O		溶于液体	-80℃(避光)	六个月
分子量：	399.49			-20℃(避光)	一个月
化学名：
Solubility (25°C)	体外	DMSO	3mg/mL warmed with 50ºC water bath (7.5mM)
		Ethanol	2mg/mL warmed with 50ºC water bath (5.0mM)
		Water	Insoluble
	体内（现配现用）
＜1mg/ml表示微溶或不溶。
普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。

制备储备液

浓度溶液体积质量	1mg	5mg	10mg
1mM	2.5032mL	12.5160mL	25.0319mL
5mM	0.5006mL	2.5032mL	5.0064mL
10mM	0.2503mL	1.2516mL	2.5032mL

生物活性

产品描述	一种选择性的骨形态发生蛋白（BMP）信号通路抑制剂。
靶点/IC50	ALK2	ALK3		ALK6	AMPK (Cell-free assay)
					109nM(Ki)
体外研究	Dorsomorphin (compound C) (0-10μM, 18h) suppresses 2DG-induced GRP78 promoter activity in human fibrosarcoma HT1080 cells in a dose-dependent manner but has little effect on tunicamycin-induced GRP78 promoter activity.Dorsomorphin (compound C) C also suppresses GRP78 promoter activity induced by glucose withdrawal. Dorsomorphin (compound C) has no effect on 2DG-induced PERK activation and reduces the both basal and 2DG-induced AMPK phosphorylation levels in HT1080 cells. Western Blot Analysis
	Cell Line:		Human fibrosarcoma HT1080 cells
	Concentration:		0-10μM.
	Incubation Time:		18 hours.
	Result:		Suppressed 2DG-induced GRP78 promoter activity in a dose-dependent manner and also suppressed GRP78 promoter activity induced by glucose withdrawal.
体内研究	Dorsomorphin (compound C: 10mg/kg, intravenously once) treatment leads to a 60% increase in total serum iron concentrations, reduces basal levels of hepcidin expression and increasing serum iron concentrations in adult mice.Dorsomorphin (compound C: 0.2mg/kg, I.V., 30 min before LPS injection) reduces ICAM-1 and VCAM-1 expression in LPSinjected rat aorta.Dorsomorphin (compound C; 25mg/kg; i.p. injection; in male BALB/c mice) treatment before lipopolysaccharide (LPS) injection significantly reduces lethality in contrast to animals treated with LPS challenge only.
	Animal Model:		Wild-type (WT) C57BL/6 adult mice that are fed a standard iron-replete diet express high levels of hepcidin.
	Dosage:		10mg/kg.
	Administration:		Intravenously once.
	Result:		Led to a 60% increase in total serum iron concentrations.Effective in reducing basal levels of hepcidin expression and increasing serum iron concentrations in adult mice.

	Animal Model:		Male Sprague-Dawley rats, 8 weeks of age (body weight 230-250g).
	Dosage:		0.2mg/kg.
	Administration:		I.V., 30 min before LPS injection.
	Result:		Reduced ICAM-1 and VCAM-1 expression in LPS-injected rat aorta.

	Animal Model:		Male BALB/c mice at 6-7 weeks of age weighing 20-22g
	Dosage:		25mg/kg
	Administration:		Injection i.p.; 60 min before LPS challenge
	Result:		Treatment of mice with 25mg/kg before LPS injection significantly reduced lethality in contrast to animals treated with LPS challenge only.

推荐实验方法(仅供参考)

激酶实验：

AMPK部分纯化和体外激酶试验

来自雄性SD大鼠的肝脏AMPK被部分纯化，进行到蓝色-琼脂糖步骤。100-μl反应混合物包含100μM AMP，100μM ATP (0.5 μCi 33P-ATP每个反应)，和50μM SAMS，以及缓冲液(40mM HEPES，pH 7.0，80mM NaCl，0.8mM EDTA，5mM MgCl2，0.025% BSA，和0.8mM DTT)。加入酶起始反应。在30°C下培育30分钟后，加入80μl 1% H3PO4停止反应。等份试样(100μl)转移到96孔MultiScreen板。板用1% H3PO4清洗3次，然后在Top-count上检测。通过化合物C，6-[4-(2-Piperidin-1-yl-ethoxy)-phenyl)]-3-pyridin-4-yl-pyyrazolo[1,5-a] pyrimidine得到的体外AMPK抑制数据，使用默克研究实验室的N. Thornberry编写的计算机程序最小二乘法Marquardt算法，通过非线性回归拟合到以下竞争性抑制方程式：Vi/Vo = (Km + S)/[S + Km × (1 + I/Ki)]，其中Vi为抑制的速度，Vo为初始速度，S为底物(ATP)浓度，Km为ATP的米氏常数，I为抑制剂(化合物C)浓度，Ki为化合物C的解离常数。