JDTic 2HCl

目录号: GC17624纯度: >99.00%同义词: (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

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

规格	价格	库存	数量
5mg	¥1,289.00	现货	1
10mg	¥2,026.00	现货	1
50mg	¥7,826.00	现货	1
10mM (in 1mL DMSO)	¥1,527.00	现货	1

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文献被引

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Nature
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632, 686–694 (2024)
Nature
618, 1017–1023 (2023)
Nature
610, 366–372 (2022)
Cell
187(9):2288-2304 (2024)
Cell
183(7):1867-1883 (2020)
Science
388(6745) (2025)
Science
387(6739) (2025)
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387(6734) (2025)
Cell Research
35, 97–116 (2025)
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33, 273–287 (2023)
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33, 546–561 (2023)
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33, 904–922 (2023)
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31, 1291–1307 (2021)

产品描述 Description

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.

实验参考方法 Experimental Reference Method

Cell experiment: [1]
Cell lines	HEK293 cells expressing KOPr-GFP
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.
Reaction Conditions	10 μM, 60 min
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]
Animal models	Male Wistar rats
Dosage form	Intraperitoneal injection, 3, or 10 mg/kg at 1 ml/kg, dissolved in sterile water
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.
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.
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.

产品文档 Product Documents

Purity:>99.00%

化学性质Chemical Properties

CAS 号

785835-79-2

同义词

(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

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 g/mol

溶解性

DMSO : 100 mg/mL (185.68 mM; Need ultrasonic); H<sub>2</sub>O : 50 mg/mL (92.84 mM; Need ultrasonic)

保存条件

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°C，然后在超声波浴中震荡一段时间。

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。

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