(±)-J 113397

Pricing Availability Delivery Time Qty
Cat.No. 2598 - (±)-J 113397 | C24H37N3O2 | CAS No. 217461-40-0
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)
Datasheet
Citations (1)
Literature

Biological Activity

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.

Technical Data

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 19.98 50
ethanol 19.98 50

Preparing Stock Solutions

The following data is based on the product molecular weight 399.57. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.5 mL 12.51 mL 25.03 mL
5 mM 0.5 mL 2.5 mL 5.01 mL
10 mM 0.25 mL 1.25 mL 2.5 mL
50 mM 0.05 mL 0.25 mL 0.5 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

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, supplier, Potent, selective, NOP, antagonists, Nociceptin, Receptors, ORL1, OP4, Opioid, J113397, NOP, Receptors, 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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