JDTic 2HClκ-opioid receptor antagonist CAS# 785835-79-2 |
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Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
| Cas No. | 785835-79-2 | SDF | Download SDF |
| PubChem ID | 66576991 | Appearance | Powder |
| Formula | C28H41Cl2N3O3 | M.Wt | 538.55 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | DMSO : 100 mg/mL (185.68 mM; Need ultrasonic) H2O : 50 mg/mL (92.84 mM; Need ultrasonic) | ||
| 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 | ||
| 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 | ||
| Standard InChIKey | QJNHURYCTCUGHH-AVWZHOAASA-N | ||
| Standard InChI | InChI=1S/C28H39N3O3.2ClH/c1-18(2)26(30-27(34)25-13-20-8-9-24(33)12-21(20)15-29-25)17-31-11-10-28(4,19(3)16-31)22-6-5-7-23(32)14-22;;/h5-9,12,14,18-19,25-26,29,32-33H,10-11,13,15-17H2,1-4H3,(H,30,34);2*1H/t19-,25+,26+,28+;;/m0../s1 | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | JDTic is a selective inhibitor of kappa opioid receptor with IC50 value of 0.02 nM. | |||||
| Targets | kappa opioid receptor | |||||
| IC50 | 0.02 nM | |||||
| 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. |
| Reacting condition | 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 |
| Application | 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. | |
JDTic 2HCl Dilution Calculator
JDTic 2HCl Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 1.8568 mL | 9.2842 mL | 18.5684 mL | 37.1368 mL | 46.4209 mL |
| 5 mM | 0.3714 mL | 1.8568 mL | 3.7137 mL | 7.4274 mL | 9.2842 mL |
| 10 mM | 0.1857 mL | 0.9284 mL | 1.8568 mL | 3.7137 mL | 4.6421 mL |
| 50 mM | 0.0371 mL | 0.1857 mL | 0.3714 mL | 0.7427 mL | 0.9284 mL |
| 100 mM | 0.0186 mL | 0.0928 mL | 0.1857 mL | 0.3714 mL | 0.4642 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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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.
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