| Identification | Back Directory | [Name]
JTC 801 | [CAS]
244218-51-7 | [Synonyms]
CS-161
JTC 801
JTC 801 HCl
JTC-801/JTC801
JTC 801 USP/EP/BP
JTC-801 >=98% (HPLC)
JTC-801 hydrochloride
N-(4-Amino-2-methyl-6-quinolinyl)-2-[(4-ethylphenoxy)methyl]benzamidehydrochloride
N-(4-AMino-2-Methyl-quinolin-6-yl)-2-(4-ethyl-phenoxyMethyl)-benzaMide hydrochloride
Benzamide,N-(4-amino-2-methyl-6-quinolinyl)-2-[(4-ethylphenoxy)methyl]-, hydrochloride
N-(4-Amino-2-methyl-6-quinolinyl)-2-[(4-ethylphenoxy)methyl]benzamide monohydrochloride | [Molecular Formula]
C26H25N3O2.ClH | [MDL Number]
MFCD06198707 | [MOL File]
244218-51-7.mol | [Molecular Weight]
447.963 |
| Chemical Properties | Back Directory | [Melting point ]
235℃ | [storage temp. ]
Inert atmosphere,2-8°C | [solubility ]
DMSO: ≥20mg/mL | [form ]
powder | [color ]
tan | [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 | [InChIKey]
NQLIYKXNAXKMBL-UHFFFAOYSA-N | [SMILES]
C(=O)(C1C=CC=CC=1COC1C=CC(CC)=CC=1)NC1C=CC2=NC(C)=CC(N)=C2C=1.Cl |
| Safety Data | Back Directory | [Hazard Codes ]
Xi | [Risk Statements ]
36 | [Safety Statements ]
26 | [WGK Germany ]
1 | [Storage Class]
11 - Combustible Solids | [Hazard Classifications]
Eye Irrit. 2 |
| Hazard Information | Back Directory | [Uses]
JTC 801 is a novel opioid receptor-like1 (ORL1) receptor antagonist. | [Biological Activity]
High affinity, selective NOP receptor antagonist (K i = 8.2 nM). Displays approximately 12.5-, 129- and 1055-fold selectivity over human μ -, κ - and δ -opioid receptors respectively. In vivo shows anti-nociceptive effects in acute pain models. Orally active. | [in vivo]
JTC-801 (≥0.01?mg/kg, i.v. or 1?mg/kg, p.o.) antagonizes the nociceptin-induced allodynia in mice. In mouse hot-plate test, JTC-801 prolongs escape response latency (ERL) to exposed heat stimulus with minimum effective doses (MED) of 0.01?mg/kg by i.v. or 1?mg/kg by p.o. In the rat formalin test, JTC-801 reduces both the first and second phases of the nociceptive response with MED of 0.01?mg/kg by i.v. administration or 1?mg/kg by p.o. administration. This anti-nociceptive action of JTC-801 is not inhibited by naloxone (10?mg/kg, s.c.). JTC-801 antagonizes the ORL1 receptor response, and has efficacious and potent anti-nociceptive effects in acute pain animal models not only by intravenous injection but also oral administration[1]. JTC-801 (0.3 mg/kg) decreases allodynia induced by the intrathecal injection of nociceptin in mice[2]. JTC-801 (6 mg/kg i.p., once daily) reverses SPS-induced mechanical allodynia, thermal hyperalgesia, anxiety-like behaviour and hypocortisolism. JTC-801 treatment also reverses NOP receptor protein and mRNA up-regulation in amygdala and PAG. JTC-801 blocks elevated N/OFQ levels in serum, CSF, PAG and hippocampus at day 21 of SPS[3]. JTC-801 (0.05-5 mg/kg, i.p.) supresses the the analgesic effect of N2O in 129Sv mice by the writhing test and tail flick test[4]. | [IC 50]
NOP Receptor/ORL1 | [storage]
Desiccate at RT |
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