JTC-801 HCl

Alias: JTC-801; JTC 801; JTC801HCl
Cat No.:V1275 Purity: ≥98%
JTC-801 HCl (JTC 801; JTC801), the hydrochloride salt of JTC801, is a potent, orally bioactive and selective opioid receptor-like1 (ORL1) receptor antagonist with potential analgesic activity.
JTC-801 HCl Chemical Structure CAS No.: 244218-51-7
Product category: Opioid Receptor
This product is for research use only, not for human use. We do not sell to patients.
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

JTC-801 HCl (JTC 801; JTC801), the hydrochloride salt of JTC801, is a potent, orally bioactive and selective opioid receptor-like1 (ORL1) receptor antagonist with potential analgesic activity. It blocks opioid receptor-like1 (ORL1) with an IC50 of 94 nM.

Biological Activity I Assay Protocols (From Reference)
Targets
NOP Receptor/ORL1
ln Vitro

In vitro activity: JTC-801 exhibits selectivity for the ORL1 receptor (Ki = 8.2 nM) over the μ, κ, and δ opioid receptors by approximately 12.5, 129, and 1055 folds, respectively. In human ORL1 receptor-expressing HeLa cells, JTC-801 does not inhibit the accumulation of cyclic AMP stimulated by forskolin; however, it does inhibit the accumulation of cyclic AMP inhibited by nociceptin, suggesting that JTC-801 has complete antagonistic activity.[2] JTC-801 inhibits the μ-receptor with an IC50 of 1831 nM and the ORL1 receptor with an IC50 of 472 nM in the rat cerebrocortical membrane. With an IC50 of 2.58 μM, JTC-801 completely counteracts the suppression of nociceptin on forskolin-induced cyclic AMP accumulation in HeLa cells expressing the ORL1 receptor.[1]

ln Vivo
JTC-801 (0.3–3 mg/kg) administered orally counteracts nociceptin-induced allodynia in mice and exhibits analgesic effects in rats and mice in a formalin test and hot plate test.[2] JTC-801 prolongs the exposed heat stimulus or escape response latency (ERL) in the mouse hot-plate test at minimum effective doses (MED) of 0.01 mg/kg by intravenous injection or 1 mg/kg by po. Using a MED of 0.01 mg/kg71 by intravenous injection or 1 mg/kg by po, JTC-801 decreases the nociceptive response in both the first and second phases in the rat formalin test.[1] In a dose-dependent manner, JTC-801 restores paw withdrawal latency (PWL). JTC-801 inhibits an increase in osteoclast numbers but not the decline in bone mineral content (BMC) or bone mineral density (BMD) brought on by a chronic constriction injury (CCI).[3] Both systemic (3-30 mg/kg) and spinal (22.5 and 45 pg) JTC-801 reverse tactile allodynia caused by L5/L6 spinal nerve ligation in a dose-dependent manner. Moreover, Fos-like immunoreactivity in the spinal cord's dorsal horn (laminae I/II) is decreased by systemic JTC-801.[4] JTC-801 has an ED50 of 0.83 mg/kg and 1.02 mg/kg for mechanical and cold anti-allodynic effects, respectively, that are dose-dependent.[6]
Enzyme Assay
Membranes from human μ-opioid receptor-expressing CHO-K1 cells suspended in 50 mM Tris-HCl buffer (pH 7.4) with 10% sucrose, 5 mM MgCl2, and 0.33 nM 2H-labeled diprenorphine are incubated for 2.5 hours at room temperature with different concentrations of JTC-801. Whatman 934-AH is used to filter the membranes, and a TopCount A9912V scintillation counter is used to count radioactivity. 10 μM naloxone is used to measure nonspecific binding (6.4%). By deducting nonspecific binding from total binding, specific binding is computed. The mean±SE (n=3) is the data.
Animal Protocol
The anti-nociceptive effect of JTC-801 and morphine is tested using the formalin stimulation test to determine the antagonistic effect of naloxone, a non-specific opioid antagonist. The procedure involves injecting 50 μL of 5% formalin subcutaneously into each rat's left hind limb to cause a licking response. Immediately following the formalin injection, the first five minutes are referred to as the first phase, and the next 15 minutes are referred to as the second phase. A measure of pain is taken of how long a limb is licked during each phase. Naloxone (10 mg/kg) dissolved in physiological saline is administered subcutaneously fifteen minutes prior to the formalin injection. JTC-801 and morphine, dissolved in 5% sorbitol and injected into the tail vein at doses of 0.03 and 1.0 mg/kg, respectively, five minutes prior to the formalin injection. An oral dose of 3.0 mg/kg of JTC-801 and 30 mg/kg of morphine is given 60 minutes prior to the formalin injection.
References

[1]. Br J Pharmacol . 2002 Jan;135(2):323-32.

[2]. J Med Chem . 2000 Nov 30;43(24):4667-77.

[3]. Neurosci Lett . 2003 Nov 20;351(3):133-6.

[4]. Eur J Pharmacol . 2005 Mar 14;510(3):223-8.

[5]. Neuropeptides . 2007 Aug;41(4):239-47.

[6]. Pharmacol Biochem Behav . 2011 Oct;99(4):540-4.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C26H26CLN3O2
Molecular Weight
447.96
Exact Mass
447.17
Elemental Analysis
C, 69.71; H, 5.85; Cl, 7.91; N, 9.38; O, 7.14
CAS #
244218-51-7
Appearance
Solid powder
SMILES
CCC1=CC=C(C=C1)OCC2=CC=CC=C2C(=O)NC3=CC4=C(C=C(N=C4C=C3)C)N.Cl
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
Chemical Name
N-(4-amino-2-methylquinolin-6-yl)-2-[(4-ethylphenoxy)methyl]benzamide;hydrochloride
Synonyms
JTC-801; JTC 801; JTC801HCl
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: 90~100 mg/mL (200.9~223.2 mM)
Water:< 1 mg/mL
Ethanol: ~31 mg/mL (~69.2 mM)
Solubility (In Vivo)
0.5% methylcellulose: 30 mg/mL
 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.2323 mL 11.1617 mL 22.3234 mL
5 mM 0.4465 mL 2.2323 mL 4.4647 mL
10 mM 0.2232 mL 1.1162 mL 2.2323 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

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Biological Data
  • JTC-801


    Effect of JTC-801 (a,b) and morphine (c,d) in the rat formalin test.Br J Pharmacol.2002 Jan;135(2):323-32.
  • JTC-801
    Mode of inhibition of JTC-801 on human ORL1 receptor.Br J Pharmacol.2002 Jan;135(2):323-32.
  • JTC-801
    Effect of JTC-801 (a,b) and morphine (c,d) in the mouse hot plate test.Br J Pharmacol.2002 Jan;135(2):323-32.
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