WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 522475
CAS#: 244218-51-7 (free base).
Description: JTC-801 is an opioid analgesic drug used in scientific research. JTC-801 is a selective antagonist for the nociceptin receptor, also known as the ORL-1 receptor. The noiciceptin receptor has complex effects which are involved in many processes involved in pain and inflammation responses, and activation of this receptor can either increase or reduce pain depending on dose. Drugs acting at the noiciceptin receptor may influence the effects of traditional analgesics such as NSAIDs, μ-opioid agonists, and cannabinoids. JTC-801 is an orally active drug that blocks the nociceptin receptor and produces analgesic effects in a variety of animal studies, and is particularly useful for neuropathic pain and allodynia associated with nerve injury.
MedKoo Cat#: 522475
Name: JTC-801 HCl
CAS#: 244218-51-7 (free base).
Chemical Formula: C26H26ClN3O2
Exact Mass:
Molecular Weight: 447.963
Elemental Analysis: C, 69.71; H, 5.85; Cl, 7.91; N, 9.38; O, 7.14
Synonym: JTC-801; JTC 801; JTC801; JTC-801 HCl.
IUPAC/Chemical Name: N-(4-Amino-2-methyl-6-quinolinyl)-2-[(4-ethylphenoxy)methyl]benzamide hydrochloride
InChi Key: NQLIYKXNAXKMBL-UHFFFAOYSA-N
InChi Code: InChI=1S/C26H25N3O2.ClH/c1-3-18-8-11-21(12-9-18)31-16-19-6-4-5-7-22(19)26(30)29-20-10-13-25-23(15-20)24(27)14-17(2)28-25;/h4-15H,3,16H2,1-2H3,(H2,27,28)(H,29,30);1H
SMILES Code: O=C(NC1=CC=C2N=C(C)C=C(N)C2=C1)C3=CC=CC=C3COC4=CC=C(CC)C=C4.[H]Cl
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
The following data is based on the product molecular weight 447.963 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 | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
1: Zhang Y, Simpson-Durand CD, Standifer KM. Nociceptin/orphanin FQ peptide receptor antagonist JTC-801 reverses pain and anxiety symptoms in a rat model of post-traumatic stress disorder. Br J Pharmacol. 2015 Jan;172(2):571-82. doi: 10.1111/bph.12701. Epub 2014 Jul 1. PubMed PMID: 24666365; PubMed Central PMCID: PMC4292969.
2: Koyama T, Fukuda K. Nociceptin receptor antagonist JTC-801 inhibits nitrous oxide-induced analgesia in mice. J Anesth. 2009;23(2):301-3. doi: 10.1007/s00540-009-0739-2. Epub 2009 May 15. PubMed PMID: 19444578.
3: Rawls SM, Schroeder JA, Ding Z, Rodriguez T, Zaveri N. NOP receptor antagonist, JTC-801, blocks cannabinoid-evoked hypothermia in rats. Neuropeptides. 2007 Aug;41(4):239-47. Epub 2007 May 23. PubMed PMID: 17512052.
4: Tamai H, Sawamura S, Takeda K, Orii R, Hanaoka K. Anti-allodynic and anti-hyperalgesic effects of nociceptin receptor antagonist, JTC-801, in rats after spinal nerve injury and inflammation. Eur J Pharmacol. 2005 Mar 14;510(3):223-8. PubMed PMID: 15763246.
5: Sestili I, Borioni A, Mustazza C, Rodomonte A, Turchetto L, Sbraccia M, Riitano D, Del Giudice MR. A new synthetic approach of N-(4-amino-2-methylquinolin-6-yl)-2-(4-ethylphenoxymethyl)benzamide (JTC-801) and its analogues and their pharmacological evaluation as nociceptin receptor (NOP) antagonists. Eur J Med Chem. 2004 Dec;39(12):1047-57. PubMed PMID: 15571866.
6: Suyama H, Kawamoto M, Gaus S, Yuge O. Effect of JTC-801 (nociceptin antagonist) on neuropathic pain in a rat model. Neurosci Lett. 2003 Nov 20;351(3):133-6. PubMed PMID: 14623124.
7: Mabuchi T, Matsumura S, Okuda-Ashitaka E, Kitano T, Kojima H, Nagano T, Minami T, Ito S. Attenuation of neuropathic pain by the nociceptin/orphanin FQ antagonist JTC-801 is mediated by inhibition of nitric oxide production. Eur J Neurosci. 2003 Apr;17(7):1384-92. PubMed PMID: 12713641.
8: Yamada H, Nakamoto H, Suzuki Y, Ito T, Aisaka K. Pharmacological profiles of a novel opioid receptor-like1 (ORL(1)) receptor antagonist, JTC-801. Br J Pharmacol. 2002 Jan;135(2):323-32. PubMed PMID: 11815367; PubMed Central PMCID: PMC1573142.
