Home >> (±)-J 113397
Related Products
(±)-J 113397 NOP receptor antagonist

Catalog No.B7119
Size Price Stock Qty
10mg
$285.00
In stock
50mg
$1,198.00
In stock

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

      

Sample solution is provided at 25 µL, 10mM.

Quality Control

Quality Control & MSDS

View current batch:

Chemical structure

(±)-J 113397

(±)-J 113397 Dilution Calculator

Concentration (start)
x
Volume (start)
=
Concentration (final)
x
Volume (final)
 
 
 
C1
V1
C2
V2

calculate

(±)-J 113397 Molarity Calculator

Mass
=
Concentration
x
Volume
x
MW*
 
 
 
g/mol

calculate

Chemical Properties

Cas No. 217461-40-0 SDF Download SDF
Chemical Name 1-((3R,4R)-1-(cyclooctylmethyl)-3-(hydroxymethyl)piperidin-4-yl)-3-ethyl-1H-benzo[d]imidazol-2(3H)-one
Canonical SMILES CCN(C1=O)C2=CC=CC=C2N1[[email protected]]3([H])CCN(C[[email protected]@]3([H])CO)CC4CCCCCCC4
Formula C24H37N3O2 M.Wt 399.57
Solubility Soluble in DMSO > 10 mM Storage Desiccate at RT
Physical Appearance White solid Shipping Condition Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Background

(±)-J 113397 is a potent and selective non-peptidyl antagonist of ORL1 receptor, with a Ki value of 1.8 nM for cloned human ORL1 [1].

The ORL1 receptor is a G protein-coupled. It is structurally related to the opioid receptors. The heptadecapeptide nociceptin/orphanin FQ is the endogenous ligand [2].

In CHO-ORL1 cells, nociceptinr/orphanin FQ dose-dependently suppressed the accumulation of cyclic AMP stimulated by forskolin with an EC value of 0.22 ± 0.011 nM. Treatment with J-113397 at increasing concentration shifted the concentration-response curve of nociceptinr/orphanin FQ to the right. Data indicated that J-113397 inhibited the interaction between nociceptinr/orphanin FQ and ORL1 in a competitive manner [1].

In a tail-flick test, an i.c.v. injection of nociceptinr/orphanin FQ at 0.01-1 nmol or saline was given to mice. I.c.v. injection of saline did not obviously change the latency of tail-flick. Nociceptinr/orphanin FQ at doses of more than 0.1 nmol shortened the latency. At the high concentration, the effect of nociceptinr/orphanin FQ reached a maximal decrease at 15 min after the injection of J-113397. The effect of nociceptinr/orphanin FQ lasted for more than 60 min. J-113397 inhibited the shortening of mouse tail-flick latency induced by nociceptinr/orphanin FQ dose-dependently. J-113397 at 30 mg/kg completely reversed the hyperalgesia elicited by nociceptinr/orphanin FQ [1].

References:
[1].  Ozaki S, Kawamoto H, Itoh Y, et al. In vitro and in vivo pharmacological characterization of J-113397, a potent and selective non-peptidyl ORL1 receptor antagonist. European journal of pharmacology, 2000, 402(1): 45-53.
[2].  Mollereau C, Mouledous L. Tissue distribution of the opioid receptor-like (ORL1) receptor. Peptides, 2000, 21(7): 907-917.