JDTic 2HCl
(Synonyms: (3R)-1,2,3,4-四氢-7-羟基-N-[(1S)-1-[[(3R,4R)-4-(3-羟基苯基)-3,4-二甲基-1-哌啶基]甲基]-2-甲基丙基]-3-异喹啉甲酰胺盐酸盐) 目录号 : GC17624
JDTic (dihydrochloride) 是一种有效的 kappa-阿片受体 (KOR) 拮抗剂，可阻断 κ-激动剂 U50, 488 诱导的镇痛作用。
Cas No.:785835-79-2
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
| Cell experiment: [1] | |
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Cell lines |
HEK293 cells expressing KOPr-GFP |
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Preparation method |
The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months. |
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Reaction Conditions |
10 μM, 60 min |
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Applications |
The compound was administered for 60 min before lysing the cells. And pJNK-ir intensities were examined by Western blot analysis. JDTic significantly increased phospho-JNK-ir at 10 μM. |
| Animal experiment: [2] | |
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Animal models |
Male Wistar rats |
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Dosage form |
Intraperitoneal injection, 3, or 10 mg/kg at 1 ml/kg, dissolved in sterile water |
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Applications |
Post-hoc analysis using Newman-Keuls test indicated a significant difference from baseline responding only in the JDTic 10 mg/kg pretreated group at the 2 h pretreatment time point (p=0.002). Furthermore, there was also a significant decrease observed in the 10 mg/kg JDTic treated group when compared to vehicle control at the 2 h time point, while the groups were virtually identical at later time points. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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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. | |
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.
| Cas No. | 785835-79-2 | SDF | |
| 别名 | (3R)-1,2,3,4-四氢-7-羟基-N-[(1S)-1-[[(3R,4R)-4-(3-羟基苯基)-3,4-二甲基-1-哌啶基]甲基]-2-甲基丙基]-3-异喹啉甲酰胺盐酸盐 | ||
| 化学名 | (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 | ||
| 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 | ||
| 分子式 | C28H41Cl2N3O3 | 分子量 | 538.55 |
| 溶解度 | DMSO : 100 mg/mL (185.68 mM; Need ultrasonic); H2O : 50 mg/mL (92.84 mM; Need ultrasonic) | 储存条件 | Store at -20°C |
| General tips | 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。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.8568 mL | 9.2842 mL | 18.5684 mL |
| 5 mM | 0.3714 mL | 1.8568 mL | 3.7137 mL |
| 10 mM | 0.1857 mL | 0.9284 mL | 1.8568 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。