JDTic
Based on 3 publication(s) in Google Scholar
JDTic is a blood-brain barrier-permeable κ-opioid receptor antagonist (Ki=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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- No. CAS: 361444-66-8
- Fòrmula: C28H39N3O3
- Peso molecular:465.63
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Almacenamiento:
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Publications Citing Use of MedChemExpress (MCE) JDTic
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Actividad biológica
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κ Opioid Receptor/KOR 0.02 nM (Ki) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | EC50 |
120 nM
Compound: 3, JDTic
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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
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[PMID: 20568781] |
| CHO | EC50 |
380 nM
Compound: 3, JDTic
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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
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[PMID: 20568781] |
| CHO | EC50 |
6 nM
Compound: 3, JDTic
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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
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[PMID: 20568781] |
| HEK293 | EC50 |
5 nM
Compound: JDTic
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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
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[PMID: 17702750] |
JDTic has a Ki 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 Ki 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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 361444-66-8
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Peso molecular 465.63
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Fòrmula C28H39N3O3
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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
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (3)
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Journal Impact Factor
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Most Recent
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Nat Chem Biol
2025 Jul;21(7):1046-1057. PMID: 39775170 -
Sci Adv
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
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Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
JDTic Related Classifications
HY-10486 Related Classifications
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