2. GPCR/G Protein Neuronal Signaling
  3. Opioid Receptor
  4. J-113397

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.

For research use only. We do not sell to patients.

J-113397 Chemical Structure

J-113397 Chemical Structure

CAS No. : 256640-45-6

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5 mg USD 498 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of J-113397:

J-113397 Related Antibodies

Top Publications Citing Use of Products

View All Opioid Receptor Isoform Specific Products:

View All Isoforms
μ Opioid Receptor/MOR κ Opioid Receptor/KOR δ Opioid Receptor/DOR NOP Receptor/ORL1

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1].

IC50 & Target

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)

In Vitro

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.

J-113397 Related Antibodies

Cell Viability Assay[1]

Cell Line: CHO-ORL1 cells
Concentration: 0, 0.1, 1, 10, 100, 200, 500 nM
Incubation Time: 10 min
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.
In Vivo

J-113397 (0-30 mg/kg; subcutaneously (s.c.); once) dose-dependently inhibits hyperalgesia elicited by intracerebroventricular (i.c.v.) administration of NociceptinNociceptin/orphanin FQ (HY-P0183) in a tail-flick test with mice[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male ICR mice (15–25 g)[1]
Dosage: 0, 3, 10, 30 mg/kg
Administration: Subcutaneously (s.c.), 10 min prior to administering 0.1 nmol nociceptin/orphanin FQ to the mice
Result: Dose-dependently inhibited hyperalgesia elicited by intracerebroventricular (i.c.v.) administration of nociceptin/orphanin FQ in a tail-flick test with mice.
Molecular Weight

399.57

Formula

C24H37N3O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1N([C@H]2[C@@H](CN(CC2)CC3CCCCCCC3)CO)C4=CC=CC=C4N1CC
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the 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.

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This equation is commonly abbreviated as: C1V1 = C2V2

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
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Working solution concentration: mg/mL
Purity & Documentation
References

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
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J-113397 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

J-113397256640-45-6J113397J 113397Opioid ReceptorNociceptinorphanin FQORL1 receptorOpioidCHO cellsGTPγShyperalgesiaInhibitorinhibitorinhibit

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