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Description: Potent and selective NOP antagonist
Chemical Name: (±)-1-[(3R*,4R*)-1-(Cyclooctylmethyl)-3-(hydroxymethyl)-4-piperidinyl]-3-ethyl-1,3-dihydro-2H-benzimidazol-2-one
Purity: ≥98% (HPLC)
Biological Activity for (±)-J 113397
(±)-J 113397 is a potent and selective NOP receptor antagonist (IC50 values are 2.3, 1400, 2200 and > 10000 nM for NOP, κ, μ and δ-opioid receptors respectively). Inhibits nociceptin/orphanin FQ-induced hyperalgesia in the mouse tail-flick test.
Compound Libraries for (±)-J 113397
(±)-J 113397 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for (±)-J 113397
| M. Wt | 399.57 |
| Formula | C24H37N3O2 |
| Storage | Desiccate at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 217461-40-0 |
| PubChem ID | 90488772 |
| InChI Key | NLSVMRCGZVSAFK-SDNSQTLOSA-N |
| Smiles | CCN1C4=C(C=CC=C4)N([C@@H]2CCN(CC3CCCCCCC3)C[C@H]2CO)C1=O.CCN5C8=C(C=CC=C8)N([C@H]6CCN(CC7CCCCCCC7)C[C@@H]6CO)C5=O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for (±)-J 113397
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 19.98 | 50 | |
| ethanol | 19.98 | 50 |
Preparing Stock Solutions for (±)-J 113397
The following data is based on the product molecular weight 399.57. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.5 mM | 5.01 mL | 25.03 mL | 50.05 mL |
| 2.5 mM | 1 mL | 5.01 mL | 10.01 mL |
| 5 mM | 0.5 mL | 2.5 mL | 5.01 mL |
| 25 mM | 0.1 mL | 0.5 mL | 1 mL |
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Product Datasheets for (±)-J 113397
References for (±)-J 113397
References are publications that support the biological activity of the product.
Kawamoto et al (1999) Discovery of the first potent and selective small molecule opioid receptor-like (ORL1) antagonist: 1-[(3R,4R)-1-cyclooctylmethyl-3-hydroxymethyl-4-piperidyl]-3-ethyl-1,3-dihydro-2H-benzimidazol-2-one (J-113397). J.Med.Chem. 42 5061 PMID: 10602690
Ozaki et al (2000) In vitro and in vivo pharmacological characterization of J-113397, a potent and selective non-peptidyl ORL1 receptor antagonist. Eur.J.Pharmacol. 402 45 PMID: 10940356
Marti et al (2007) The nociceptin/orphanin FQ receptor antagonist J-113397 and L-DOPA additively attenuate experimental Parkinsonism through overinhibition of nigrothalamic pathway. J.Neurosci. 27 1297 PMID: 17287504
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Keywords: (±)-J 113397, (±)-J 113397 supplier, Potent, selective, NOP, antagonists, Nociceptin, Receptors, ORL1, OP4, Opioid, J113397, 2598, Tocris Bioscience
1 Citation for (±)-J 113397
Citations are publications that use Tocris products. Selected citations for (±)-J 113397 include:
Wen et al (2011) Pharmacological mechanisms underlying the antinociceptive and tolerance effects of the 6,14-bridged oripavine compound 030418. Acta Pharmacol Sin 32 1215 PMID: 21863064
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