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Art. -Nr.: HY-10486

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JDTic

3 Cited Publications

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Based on 3 publication(s) in Google Scholar

JDTic is a blood-brain barrier-permeable κ-opioid receptor antagonist (K_i=0.02 nM) with favorable in vitro ADME properties. JDTic blocks agonist-mediated Gi and β-arrestin signaling pathways as well as analgesic effects by stabilizing the inactive conformation of hKOR and activating JNK. JDTic may also induce transient asymptomatic ventricular tachycardia. JDTic is widely applicable to studies related to depression, anxiety, stress-induced addictive behaviors, and nicotine withdrawal.

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CAS. Nr.: 361444-66-8
Formel: C₂₈H₃₉N₃O₃
Molecular Weight:465.63

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (270 KB)

JDTic Chemical Structure

CAS. Nr.: 361444-66-8

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Use of MCE Products

Fluorescent Dye

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Clinical Trial
Chemical Information
Publications (3)
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

κ Opioid Receptor/KOR

0.02 nM (Ki)

Alle Opioid Receptor Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	EC₅₀	120 nM Compound: 3, JDTic	Agonist activity at human recombinant mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay Agonist activity at human recombinant mu opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay	[PMID: 20568781]
CHO	EC₅₀	380 nM Compound: 3, JDTic	Agonist activity at human recombinant delta opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay Agonist activity at human recombinant delta opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay	[PMID: 20568781]
CHO	EC₅₀	6 nM Compound: 3, JDTic	Agonist activity at human recombinant kappa opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay Agonist activity at human recombinant kappa opioid receptor expressed in CHO cells by [35S]GTPgammaS binding assay	[PMID: 20568781]
HEK293	EC₅₀	5 nM Compound: JDTic	Increase of JNK phosphorylation in U50488 treated HEK293 cells expressing GFP tagged kappa opioid receptor Increase of JNK phosphorylation in U50488 treated HEK293 cells expressing GFP tagged kappa opioid receptor	[PMID: 17702750]

In Vitro

JDTic has a K_i value of 0.02 nM for the κ receptor, with 1255-fold selectivity over the μ receptor and 3800-fold selectivity over the δ receptor^[1].
JDTic inhibits binding to the human hERG potassium channel, with a K_i value of 8.820 μM^[1].
JDTic shows no agonist activity in HEK293-T cells and can completely inhibit the signaling pathway induced by U69593^[3].

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

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 361444-66-8
Molecular Weight 465.63
Formel C₂₈H₃₉N₃O₃
SMILES

O=C([C@@H]1NCC2=C(C=CC(O)=C2)C1)N[C@@H](C(C)C)CN3C[C@H](C)[C@](C)(C4=CC=CC(O)=C4)CC3
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Publications (3)

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Nat Chem Biol

Molecular mechanisms of inverse agonism via κ-opioid receptor-G protein complexes. [Abstract]

2025 Jul;21(7):1046-1057. PMID: 39775170
Sci Adv

Structure-based design of an opioid receptor modulator for enhanced morphine analgesia. [Abstract]

2026 Feb 13;12(7):eaea9832. PMID: 41671375
Neuropharmacology

GPR88 impairs the signaling of kappa opioid receptors in a heterologous system and in primary striatal neurons. [Abstract]

2025 Mar 1:265:110242. PMID: 39613254

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (270 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]. Carroll FI, et al. Design, synthesis, and pharmacological evaluation of JDTic analogs to examine the significance of the 3- and 4-methyl substituents. Bioorg Med Chem. 2015;23(19):6379-6388. [Content Brief]

[2]. Chavkin C, et al. Kappa antagonist JDTic in phase 1 clinical trial[J]. Neuropsychopharmacology, 2015, 40(9): 2057-2058.

[3]. Wu H, et al. Structure of the human κ-opioid receptor in complex with JDTic[J]. Nature, 2012, 485(7398): 327-332.

Calculators

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)}

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.

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MOQ

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100 mg

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- Clinical Trial
Chemical Information
Publications (3)
Reinheit & Dokumentation
Verweise

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JDTic

Publications Citing Use of MedChemExpress (MCE) JDTic

Alle Opioid Receptor Isoform-spezifische Produkte anzeigen