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JDTic 2HCl

现货
Catalog No.
A3518
κ-阿片受体拮抗剂
组合的产品项目
规格价格库存 数量
5mg
¥ 1,720.00
Ship with 10-15 days
10mg
¥ 2,700.00
Ship with 10-15 days
50mg
¥ 10,430.00
Ship with 10-15 days

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Background

JDTic is a selective inhibitor of kappa opioid receptor with IC50 value of 0.02nM [1].

JDTic is one of the kappa opioid receptor selective antagonists. These antagonists are thought as potential pharmacotherapies for addiction, anxiety disorders, depression, psychosis disorders and obesity. Because of the unique structural feature of JDTic, it is more selective and potent for KOR activity than other KOR antagonists. JDTic is shown to block the antinociceptive response of nicotine in the tail-flick test with a dose-dependent manner. It (8 mg/kg) can also block the nicotine withdrawal signs in mice via effecting the expression of a CPA associated with nicotine withdrawal. Additionally, JDTic is also reported to decrease the number of somatic withdrawal signs in morphine-dependent rats [2,3].

References:
[1] Michael P. Hedrick, Palak Gosalia, Kelin Li, Kevin Frankowski, Shenghua Shi, Thomas E. Prisinzano, Frank Schoenen, Jeffrey Aubé, Ying Su, S. Vasile, Eduard Sergienko, Wilson Gray, Santosh Hariharan, Loribelle Milan, Susanne Heynen-Genel, Bryan L. Roth, Jon Evans, Vincent Setola, Thomas D.Y. Chung, Marc Caron, Laura M. Bohn and Lawrence S. Barak. Antagonist for the Kappa Opioid Receptor. Molecular Libraries. 2011 Jun: 1-32.
[2] Scott P. Runyon, Lawrence E. Brieaddy, S. Wayne Mascarella, James B. Thomas, Hernán A. Navarro, James L. Howard, Gerald T. Pollard, and F. Ivy Carroll. Analogues of (3R)-7-Hydroxy-N-[(1S)-1-{[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethyl-1-piperidinyl]methyl}-2-methylpropyl)-1,2,3,4-tetrahydro-3-isoquinolinecarboxamide(JDTic). Synthesis and In Vitro and In Vivo Opioid Receptor Antagonist Activity. J Med Chem. 2010 July, 53(14): 5290–5301.
[3] K. J. Jackson, Frank Ivy Carroll, S. S. Negus and M. I. Damaj. Effect of the selective kappa-opioid receptor antagonist JDTic on nicotine antinociception, reward, and withdrawal in the mouse. Psychopharmacology (Berl). 2010 June, 210(2): 285–294.

Chemical Properties

StorageStore at -20°C
M.Wt538.55
Cas No.785835-79-2
FormulaC28H41Cl2N3O3
SolubilitySoluble in DMSO
Chemical Name(3R)-7-hydroxy-N-[(2S)-1-[(3R,4R)-4-(3-hydroxyphenyl)-3,4-dimethylpiperidin-1-yl]-3-methylbutan-2-yl]-1,2,3,4-tetrahydroisoquinoline-3-carboxamide dihydrochloride
SDFDownload SDF
Canonical SMILESCC1CN(CCC1(C)C2=CC(=CC=C2)O)CC(C(C)C)NC(=O)C3CC4=C(CN3)C=C(C=C4)O.Cl.Cl
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验[1]:

细胞系

表达KOPr-GFP的HEK293细胞

溶解方法

该化合物在DMSO中的溶解度大于10 mM。若配制更高浓度的溶液,一般步骤如下:请将试管置于37℃加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20℃可放置数月

反应条件

10 μM,60 min

实验结果

在裂解细胞之前使用JDTic处理60分钟,通过Western印迹分析检查pINK-ir强度,10 μM的JDTic显著增加磷酸化JNK-ir。

动物实验[2]:

动物模型

雄性Wistar大鼠

剂量

腹膜内注射,3或10 mg/kg,溶于无菌水

实验结果

Newman-Keuls实验的分析表明,10 mg/kgJDTic仅在2小时预处理时间点(p = 0.002)时与基线有显著差异。此外,与载体对照相比,在2小时时间点,在10 mg/kgJDTic处理组中观察到基线显著降低,而在稍后的时间点上基本相同。

注意事项

请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的,属于正常现象。

References:

[1] Melief E J, Miyatake M, Carroll F I, et al. Duration of action of a broad range of selective κ-opioid receptor antagonists is positively correlated with c-Jun N-terminal kinase-1 activation. Molecular pharmacology, 2011, 80(5): 920-929.

[2] Schank J R, Goldstein A L, Rowe K E, et al. The kappa opioid receptor antagonist JDTic attenuates alcohol seeking and withdrawal anxiety. Addiction biology, 2012, 17(3): 634-647.

生物活性

描述 JDTic是一种选择性的κ-阿片受体抑制剂,IC50值为0.02 nM。
靶点 kappa opioid receptor          
IC50 0.02 nM          

质量控制

质量控制和MSDS

批次:

化学结构

JDTic 2HCl