Cat. No.: HY-114072

J-113397

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Based on 1 Customer Validation

J-113397 is the first potent and selective nonpeptidyl ORL1 receptor antagonist (K_i: cloned human ORL1=1.8 nM) without any agonistic effects on other opioid receptors.

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

Purity: 99.00%
CAS No.: 256640-45-6
Formula: C₂₄H₃₇N₃O₂
Molecular Weight:399.57

Storage:

4°C, sealed storage, away from moisture

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

J-113397 Chemical Structure

CAS No.: 256640-45-6

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Solvent & Solubility
- In Vitro
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

Description

J-113397 is the first potent and selective nonpeptidyl ORL1 receptor antagonist (K_i: 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)

All Opioid Receptor Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	EC₅₀	>10 μM Compound: J-113397 (3R,4R)	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	[PMID: 10602690]
CHO	IC₅₀	1400 nM Compound: J-113397 (3R,4R)	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	[PMID: 10602690]
CHO	IC₅₀	2.3 nM Compound: J-113397 (3R,4R)	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	[PMID: 10602690]
CHO	IC₅₀	2200 nM Compound: J-113397 (3R,4R)	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	[PMID: 10602690]
CHO	IC₅₀	5.6 nM Compound: J-113397 (3R,4R)	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	[PMID: 10602690]
CHO	IC₅₀	>10000 nM Compound: J-113397 (3R,4R)	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	[PMID: 10602690]
CHO	EC₅₀	>10 μM Compound: 1	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	[PMID: 16451050]
CHO	IC₅₀	>10 μM Compound: 1	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	[PMID: 16451050]
CHO	IC₅₀	1.5 nM Compound: 1	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	[PMID: 16451050]
CHO	IC₅₀	1600 nM Compound: 1	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	[PMID: 16451050]
CHO	IC₅₀	2.4 nM Compound: 1	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	[PMID: 16451050]
CHO	IC₅₀	3400 nM Compound: 1	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	[PMID: 16451050]
CHO	IC₅₀	2.3 nM Compound: 1, J-113397	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	[PMID: 19537798]

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.

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.

Chemical Information

CAS No. 256640-45-6
Appearance Solid
Molecular Weight 399.57
Formula C₂₄H₃₇N₃O₂
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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.5027 mL

12.5135 mL

25.0269 mL

5 mM

0.5005 mL

2.5027 mL

5.0054 mL

10 mM

---

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.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Dilution Calculator

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Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Ozaki S, et al. In vitro and in vivo pharmacological characterization of J-113397, a potent and selective non-peptidyl ORL1 receptor antagonist. Eur J Pharmacol. 2000 Aug 18;402(1-2):45-53. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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
DMSO	5 mM	0.5005 mL	2.5027 mL	5.0054 mL	12.5135 mL

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J-113397

GPCR/G Protein Compound Library

Neuronal Signaling Compound Library

Neurotransmitter Receptor Compound Library

Anti-Obesity Compound Library

Pain-Related Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

All Opioid Receptor Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

J-113397

GPCR/G Protein Compound Library

Neuronal Signaling Compound Library

Neurotransmitter Receptor Compound Library

Anti-Obesity Compound Library

Pain-Related Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

All Opioid Receptor Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

J-113397 Related Classifications

Cat. No.: HY-114072