J-113397
Based on 1 Customer Validation
J-113397 is the first potent and selective nonpeptidyl ORL1 receptor antagonist (Ki: cloned human ORL1=1.8 nM) without any agonistic effects on other opioid receptors.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.95%
- No. CAS: 256640-45-6
- Fòrmula: C24H37N3O2
- Peso molecular:399.57
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Almacenamiento:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
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NOP Receptor/ORL1 1.8 ± 0.24 nM (Ki) |
κ Opioid Receptor/KOR 640 ± 87 nM (Ki) |
μ Opioid Receptor/MOR 1000 ± 160 nM (Ki) |
δ Opioid Receptor/DOR >10000 nM (Ki) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | EC50 |
>10 μM
Compound: J-113397 (3R,4R)
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Agonistic activity against nociceptin produced GTPgammaS binding to Opioid receptor like 1 expressed in CHO cells
Agonistic activity against nociceptin produced GTPgammaS binding to Opioid receptor like 1 expressed in CHO cells
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[PMID: 10602690] |
| CHO | IC50 |
1400 nM
Compound: J-113397 (3R,4R)
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Binding affinity in CHO cells stably expressing cloned human Opioid receptor kappa 1 by displacing radioligand [3H]U-69593
Binding affinity in CHO cells stably expressing cloned human Opioid receptor kappa 1 by displacing radioligand [3H]U-69593
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[PMID: 10602690] |
| CHO | IC50 |
2.3 nM
Compound: J-113397 (3R,4R)
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Binding affinity in CHO cells stably expressing cloned human Opioid receptor like 1 by displacing radioligand [125I]Tyr14-nociceptin
Binding affinity in CHO cells stably expressing cloned human Opioid receptor like 1 by displacing radioligand [125I]Tyr14-nociceptin
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[PMID: 10602690] |
| CHO | IC50 |
2200 nM
Compound: J-113397 (3R,4R)
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Binding affinity in CHO cells stably expressing cloned human Opioid receptor mu 1 by displacing diprenorphine
Binding affinity in CHO cells stably expressing cloned human Opioid receptor mu 1 by displacing diprenorphine
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[PMID: 10602690] |
| CHO | IC50 |
5.6 nM
Compound: J-113397 (3R,4R)
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Antagonistic activity against nociceptin produced [35S]GTP-gamma-S, binding to Opioid receptor like 1 expressed in CHO cells
Antagonistic activity against nociceptin produced [35S]GTP-gamma-S, binding to Opioid receptor like 1 expressed in CHO cells
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[PMID: 10602690] |
| CHO | IC50 |
>10000 nM
Compound: J-113397 (3R,4R)
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Binding affinity in CHO cells stably expressing cloned human Opioid receptor delta 1 by displacing radioligand [3H][D-Ala2,D-Leu5]enkephalin
Binding affinity in CHO cells stably expressing cloned human Opioid receptor delta 1 by displacing radioligand [3H][D-Ala2,D-Leu5]enkephalin
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[PMID: 10602690] |
| CHO | EC50 |
>10 μM
Compound: 1
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Agonist activity on nociceptin-induced maximal [35S]GTP-gamma-S binding to ORL1 expressed in CHO cells
Agonist activity on nociceptin-induced maximal [35S]GTP-gamma-S binding to ORL1 expressed in CHO cells
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[PMID: 16451050] |
| CHO | IC50 |
>10 μM
Compound: 1
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Displacement of [3H]naltrindole from cloned human delta opioid receptor expressed in CHO cells
Displacement of [3H]naltrindole from cloned human delta opioid receptor expressed in CHO cells
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[PMID: 16451050] |
| CHO | IC50 |
1.5 nM
Compound: 1
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Antagonist activity on nociceptin-induced [35S]GTP-gamma-S binding to ORL1 expressed in CHO cells
Antagonist activity on nociceptin-induced [35S]GTP-gamma-S binding to ORL1 expressed in CHO cells
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[PMID: 16451050] |
| CHO | IC50 |
1600 nM
Compound: 1
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Displacement of [3H]U-69593 from cloned human kappa opioid receptor expressed in CHO cells
Displacement of [3H]U-69593 from cloned human kappa opioid receptor expressed in CHO cells
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[PMID: 16451050] |
| CHO | IC50 |
2.4 nM
Compound: 1
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Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
Displacement of [125I]Tyr-nociceptin from cloned human ORL1 expressed in CHO cells
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[PMID: 16451050] |
| CHO | IC50 |
3400 nM
Compound: 1
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Displacement of [3H]diprenorphin from cloned human mu opioid receptor expressed in CHO cells
Displacement of [3H]diprenorphin from cloned human mu opioid receptor expressed in CHO cells
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[PMID: 16451050] |
| CHO | IC50 |
2.3 nM
Compound: 1, J-113397
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Displacement of [125I]Tyr14-nociceptin from human cloned ORL1 receptor expressed in CHO cells
Displacement of [125I]Tyr14-nociceptin from human cloned ORL1 receptor expressed in CHO cells
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[PMID: 19537798] |
J-113397 (0-500 nM) inhibits NociceptinNociceptin/orphanin FQ (HY-P0183)-stimulated [35S]GTPγS binding to CHO cells expressing ORL1 (CHO-ORL1) but had no effect on [35S]GTPγS binding by itself[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:CHO-ORL1 cells
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Concentration:0, 0.1, 1, 10, 100, 200, 500 nM
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Incubation Time:10 min
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Result:Inhibited nociceptin/orphanin FQ-stimulated [35S]guanosine 5′-O-(γ-thio)triphosphate (GTPγS) binding to Chinese Hamster Ovary (CHO) cells expressing ORL1 (CHO-ORL1) with an IC50 value of 5.3 nM but had no effect on [35S]GTPγS binding by itself.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male ICR mice (15–25 g)[1]
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Dosage:0, 3, 10, 30 mg/kg
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Administration:Subcutaneously (s.c.), 10 min prior to administering 0.1 nmol nociceptin/orphanin FQ to the mice
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Result:Dose-dependently inhibited hyperalgesia elicited by intracerebroventricular (i.c.v.) administration of nociceptin/orphanin FQ in a tail-flick test with mice.
Chemical Information
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No. CAS 256640-45-6
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Appearance Solid
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Peso molecular 399.57
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Fòrmula C24H37N3O2
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Color White to off-white
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SMILES
O=C1N([C@H]2[C@@H](CN(CC2)CC3CCCCCCC3)CO)C4=CC=CC=C4N1CC
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvente y solubilidad
DMSO : 2 mg/mL (5.01 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureza y Documentación
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Ficha de datos (279 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.5027 mL | 12.5135 mL | 25.0269 mL | 62.5673 mL |
| 5 mM | 0.5005 mL | 2.5027 mL | 5.0054 mL | 12.5135 mL |
J-113397 Related Classifications
HY-114072 Related Classifications
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