(±)-J 113397 |
رقم الكتالوجGC18090 |
(± ؛) - J 113397 هو مناهض قوي وانتقائي لمستقبلات ORL1 غير الببتيدل مع Ki 1.8 نانومتر من أجل ORL1 البشري المستنسخ.
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Cas No.: 217461-40-0
Sample solution is provided at 25 µL, 10mM.
(±)-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.
Cas No. | 217461-40-0 | 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[C@]3([H])CCN(C[C@@]3([H])CO)CC4CCCCCCC4 | ||
Formula | C24H37N3O2 | M.Wt | 399.57 |
الذوبان | <19.98mg/ml in DMSO; <19.98mg/ml in ethanol | Storage | Desiccate at RT |
General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. |
Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
1 mM | 2.5027 mL | 12.5135 mL | 25.0269 mL |
5 mM | 0.5005 mL | 2.5027 mL | 5.0054 mL |
10 mM | 0.2503 mL | 1.2513 mL | 2.5027 mL |
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