JDTic 2HCl
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
JDTic是一种选择性的κ-阿片受体抑制剂，IC50值为0.02 nM[1]。
JDTic是κ-阿片受体的选择性拮抗剂之一。这些拮抗剂被认为是有潜力的药物疗法，用于治疗成瘾、焦虑症、抑郁症、精神病障碍和肥胖症。由于其独特的结构特征，与其它KOR拮抗剂相比，JDTic对KOR活性具有更高的选择性和效力。在甩尾实验中，JDTic以剂量依赖的方式阻断尼古丁的镇痛响应。在小鼠中，JDTic（8 mg/kg）通过影响与尼古丁戒断相关的CPA的表达，从而阻断尼古丁戒断症状。此外，在吗啡依赖性大鼠中，JDTic减少躯体戒断症状的数量[2，3]。
参考文献：
[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.
| Storage | Store at -20°C |
| M.Wt | 538.55 |
| Cas No. | 785835-79-2 |
| Formula | C28H41Cl2N3O3 |
| Solubility | Soluble 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 |
| SDF | Download SDF |
| Canonical SMILES | CC1CN(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 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 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。溶液形式一般不宜长期储存，请尽快用完。 |
| 细胞实验[1]: | |
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细胞系 |
表达KOPr-GFP的HEK293细胞 |
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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 |
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反应条件 |
10 μM，60 min |
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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]: | |
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动物模型 |
雄性Wistar大鼠 |
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剂量 |
腹膜内注射，3或10 mg/kg，溶于无菌水 |
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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。 |
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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。 |
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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. | |
| 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 | |||||
化学结构
