Home Neuronal Signaling Opioid Receptor antagonist JTC-801

research use only

JTC-801 Opioid Receptor antagonist

Cat.No.S2722

JTC-801 is a selective opioid receptor-like1 (ORL1) receptor antagonist with IC50 of 94 nM, weakly inhibits receptors δ, κ, and μ.
JTC-801 Opioid Receptor antagonist Chemical Structure

Chemical Structure

Molecular Weight: 447.96

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: S272201 DMSO]90 mg/mL]false]Ethanol]31 mg/mL]false]Water]Insoluble]false Purity: 99.94%
99.94

Chemical Information, Storage & Stability

Molecular Weight 447.96 Formula

C26H25N3O2.HCl

 Storage (From the date of receipt)
CAS No. 244218-51-7 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles CCC1=CC=C(C=C1)OCC2=CC=CC=C2C(=O)NC3=CC4=C(C=C(N=C4C=C3)C)N.Cl

Solubility

In vitro
Batch:

DMSO : 90 mg/mL ( (200.91 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 31 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC50/Ki
Opioid receptor-like1 (ORL1) [1]
94 nM
In vitro
JTC-801 displays about 12.5-, 129-, and 1055-fold selectivity for ORL1 receptor (Ki = 8.2 nM) over μ-, κ-, and δ-opioid receptors, respectively. This compound does not inhibit forskolin-stimulated cyclic AMP accumulation in human ORL1 receptor-expressing HeLa cells, but it prevents nociceptin-induced inhibition of cyclic AMP accumulation, indicating that this chemical possesses full antagonistic activity. [2] In rat cerebrocortical membrane, this compound inhibits ORL1 receptor with IC50 of 472 nM and μ-receptor with IC50 of 1831 nM. It completely antagonizes the suppression of nociceptin on forskolin-induced accumulation of cyclic AMP with IC50 of 2.58 μM in HeLa cells expressing ORL1 receptor. [1]
In vivo
Oral administration of JTC-801 (0.3-3 mg/kg) antagonizes nociceptin-induced allodynia in mice, and shows analgesic effect in a hot plate test using mice and in a formalin test using rats. [2] In mouse hot-plate test, this compound prolongs escape response latency (ERL) or 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, it reduces both the first and second phases of the nociceptive response with MED of 0.01 mg/kg71 by i.v. or 1 mg/kg by p.o. [1] This chemical dose-dependently normalizes paw withdrawal latency (PWL). Although it does not inhibit a chronic constriction injury (CCI)-induced decrease in bone mineral content (BMC) and bone mineral density (BMD), it inhibits an increase in the number of osteoclasts. [3] Tactile allodynia induced by L5/L6 spinal nerve ligation is reversed by both systemic (3-30 mg/kg) and spinal (22.5 and 45 pg) administration of this compound in a dose-dependent manner. Furthermore, systemic treatment reduces Fos-like immunoreactivity in the dorsal horn of the spinal cord (laminae I/II). [4] It produces dose-dependent mechanical and cold anti-allodynic effects with ED50 of 0.83 mg/kg and 1.02 mg/kg, respectively. [6]
References
  • https://pubmed.ncbi.nlm.nih.gov/15763246/
  • https://pubmed.ncbi.nlm.nih.gov/17512052/
  • https://pubmed.ncbi.nlm.nih.gov/21664922/

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.

Signaling Pathway Map