Art. -Nr.: HY-107721

(±)-J-113397

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(±)-J-113397 is a potent and selective non-peptidyl ORL1 receptor antagonist with a K_i of 1.8 nM for cloned human ORL1. J-113397 inhibited nociceptin/orphanin FQ-stimulated GTPγS binding to CHO cells expressing ORL1 with an IC₅₀ value of 5.3 nM. J-113397 can be used for researching the physiological roles of nociceptin/orphanin FQ.

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Reinheit: 99.82%
CAS. Nr.: 217461-40-0
Formel: C₂₄H₃₇N₃O₂
Molecular Weight:399.57

Speicherung:

4°C, sealed storage, away from moisture and light

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

(±)-J-113397 Chemical Structure

CAS. Nr.: 217461-40-0

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

NOP Receptor/ORL1

Alle Opioid Receptor Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	EC₅₀	>10 μM Compound: J-112444 (3S,4S)	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	>10 μM Compound: J-112444 (3S,4S)	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	2600 nM Compound: J-112444 (3S,4S)	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	3300 nM Compound: J-112444 (3S,4S)	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	820 nM Compound: J-112444 (3S,4S)	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]

Chemical Information

CAS. Nr. 217461-40-0
Appearance Solid
Molecular Weight 399.57
Formel C₂₄H₃₇N₃O₂
Color Off-white to pink
SMILES

O=C1N([C@](CCN2CC3CCCCCCC3)([H])[C@H](C2)CO)C4=CC=CC=C4N1CC
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, sealed storage, away from moisture and light

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

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : ≥ 100 mg/mL (250.27 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

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

0.2503 mL

1.2513 mL

2.5027 mL

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 and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (6.26 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (6.26 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 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)

Verweise

[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;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
	5 mM	0.5005 mL	2.5027 mL	5.0054 mL	12.5135 mL
	10 mM	0.2503 mL	1.2513 mL	2.5027 mL	6.2567 mL
	15 mM	0.1668 mL	0.8342 mL	1.6685 mL	4.1712 mL
	20 mM	0.1251 mL	0.6257 mL	1.2513 mL	3.1284 mL
	25 mM	0.1001 mL	0.5005 mL	1.0011 mL	2.5027 mL
	30 mM	0.0834 mL	0.4171 mL	0.8342 mL	2.0856 mL
	40 mM	0.0626 mL	0.3128 mL	0.6257 mL	1.5642 mL
	50 mM	0.0501 mL	0.2503 mL	0.5005 mL	1.2513 mL
	60 mM	0.0417 mL	0.2086 mL	0.4171 mL	1.0428 mL
	80 mM	0.0313 mL	0.1564 mL	0.3128 mL	0.7821 mL
	100 mM	0.0250 mL	0.1251 mL	0.2503 mL	0.6257 mL

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(±)-J-113397

Bioactive Compound Library Max

Bioactive Compound Library

GPCR/G Protein Compound Library

Neuronal Signaling Compound Library

Neurotransmitter Receptor Compound Library

Anti-Obesity Compound Library

Heterocyclic Compound Library

Pain-Related Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

MCE Bioactive Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

Alle Opioid Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

(±)-J-113397

Bioactive Compound Library Max

Bioactive Compound Library

GPCR/G Protein Compound Library

Neuronal Signaling Compound Library

Neurotransmitter Receptor Compound Library

Anti-Obesity Compound Library

Heterocyclic Compound Library

Pain-Related Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

MCE Bioactive Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

Alle Opioid Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

(±)-J-113397 Related Classifications

HY-107721 Related Classifications