JTC 801

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Cat.No. 2481 - JTC 801 | C26H25N3O2.HCl | CAS No. 244218-51-7
Description: Selective NOP antagonist
Chemical Name: N-(4-Amino-2-methyl-6-quinolinyl)-2-[(4-ethylphenoxy)methyl]benzamide hydrochloride
Purity: ≥98% (HPLC)
Datasheet
Citations (3)
Reviews
Literature (5)

Biological Activity

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

JTC 801 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data

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

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 44.8 100
ethanol 8.96 20

Preparing Stock Solutions

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.

Select a batch to recalculate based on the batch molecular weight:
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

Certificate of Analysis / Product Datasheet
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References

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


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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:

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

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


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