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Submit ReviewJTC 801
Description: Selective NOP antagonist
Chemical Name: N-(4-Amino-2-methyl-6-quinolinyl)-2-[(4-ethylphenoxy)methyl]benzamide hydrochloride
Purity: ≥98% (HPLC)
Biological Activity for JTC 801
JTC 801 is a high affinity, selective NOP receptor antagonist (Ki = 8.2 nM). Displays approximately 12.5-, 129- and 1055-fold selectivity over human μ-, κ- and δ-opioid receptors respectively. Exhibits anti-nociceptive effects in acute pain models in vivo. Orally active.
Compound Libraries for JTC 801
JTC 801 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for JTC 801
| M. Wt | 447.96 |
| Formula | C26H25N3O2.HCl |
| Storage | Desiccate at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 244218-51-7 |
| PubChem ID | 5311339 |
| InChI Key | NQLIYKXNAXKMBL-UHFFFAOYSA-N |
| Smiles | Cl.CCC1=CC=C(OCC2=CC=CC=C2C(=O)NC2=CC3=C(N)C=C(C)N=C3C=C2)C=C1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for JTC 801
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 44.8 | 100 | |
| ethanol | 8.96 | 20 |
Preparing Stock Solutions for JTC 801
The following data is based on the product molecular weight 447.96. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.23 mL | 11.16 mL | 22.32 mL |
| 5 mM | 0.45 mL | 2.23 mL | 4.46 mL |
| 10 mM | 0.22 mL | 1.12 mL | 2.23 mL |
| 50 mM | 0.04 mL | 0.22 mL | 0.45 mL |
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Product Datasheets for JTC 801
References for JTC 801
References are publications that support the biological activity of the product.
Shinkai et al (2000) 4-Aminoquinolines: novel nociceptin antagonists with analgesic activity. J.Med.Chem 43 4667 PMID: 11101358
Yamada et al (2002) Pharmacological profiles of a novel opioid receptor-like1 (ORL1) receptor antagonist, JTC-801. Br.J.Pharmacol. 135 323 PMID: 11815367
Tamai et al (2005) Anti-allodynic and anti-hyperalgesic effects of nociceptin receptor antagonist, JTC-801, in rats after spinal nerve injury and inflammation. Eur.J.Pharmacol. 510 223 PMID: 15763246
If you know of a relevant reference for JTC 801, please let us know.
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Keywords: JTC 801, JTC 801 supplier, Selective, NOP, antagonists, Nociceptin, Receptors, ORL1, OP4, Opioids, JTC801, 2481, Tocris Bioscience
3 Citations for JTC 801
Citations are publications that use Tocris products. Selected citations for JTC 801 include:
Delaney et al (2012) Role of nociceptin/orphanin FQ and NOP receptors in the response to acute and repeated restraint stress in rats. J Neuroendocrinol 24 1527 PMID: 22835008
Mahmoud et al (2010) Modulation of silent and constitutively active nociceptin/orphanin FQ receptors by potent receptor antagonists and Na+ ions in rat sympathetic neurons. Mol Pharmacol 77 804 PMID: 20159949
Zhang et al (2015) Nociceptin/orphanin FQ peptide receptor antagonist JTC-801 reverses pain and anxiety symptoms in a rat model of post-traumatic stress disorder. PLoS One 172 571 PMID: 24666365
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