JTC-801 free base
Based on 7 publication(s) in Google Scholar
JTC-801 free base is a selective opioid receptor-like1 (ORL1) receptor antagonist, binding to ORL1 receptor with a Ki value of 8.2?nM.
For research use only. We do not sell to patients.
- CAS No.: 244218-93-7
- Formula: C26H25N3O2
- Molecular Weight:411.50
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications Citing Use of MedChemExpress (MCE) JTC-801 free base
More- Neurotherapeutics. 2024 Jul 13:e00424. [Abstract]
- Mol Biotechnol. 2025 Jan 6. [Abstract]
- J Pain Res. 2025 Jun 5:18:2775-2790. [Abstract]
- Oncol Lett. 2019 Feb;17(2):1939-1945. [Abstract]
- J Recept Signal Transduct Res. 2018 Apr;38(2):133-140. [Abstract]
- Pharmazie. 2018 May 1;73(5):283-287. [Abstract]
- Med Sci (Paris). 2018 Oct:34 Focus issue F1:8-14. [Abstract]
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All Opioid Receptor Isoforms
More
Biological Activity
Ki: 8.2?nM (ORL1)[2]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
1507 nM
Compound: JTC-801
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Displacement of [3H]-naltrindole from human mu opioid receptor expressed in CHO cells after 2 hrs by scintillation counting
Displacement of [3H]-naltrindole from human mu opioid receptor expressed in CHO cells after 2 hrs by scintillation counting
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[PMID: 21330016] |
| HEK293 | IC50 |
30 nM
Compound: JTC-801
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Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
Displacement of [125I]Tyr14-nociceptin from human NOP receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
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[PMID: 21330016] |
| HEK293 | IC50 |
7512 nM
Compound: JTC-801
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Displacement of [3H]-naltrindole from human kappa opioid receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
Displacement of [3H]-naltrindole from human kappa opioid receptor expressed in human HEK293 cells after 2 hrs by scintillation counting
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[PMID: 21330016] |
Chemical Information
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CAS No. 244218-93-7
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Molecular Weight 411.50
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Formula C26H25N3O2
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SMILES
O=C(C1=CC=CC=C1COC2=CC=C(C=C2)CC)NC3=CC=C4N=C(C=C(C4=C3)N)C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (7)
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Journal Impact Factor
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Most Recent
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Neurotherapeutics
LY2940094, an NOPR antagonist, promotes oligodendrocyte generation and myelin recovery in an NOPR independent manner. [Abstract]2024 Jul 13:e00424. PMID: 39004556 -
Mol Biotechnol
Identification and Validation of Alkaliptosis Resistance-Associated Genes in Prostate Cancer Via Transcriptome Sequencing and Prediction of Biochemical Recurrence. [Abstract]2025 Jan 6. PMID: 39760809 -
J Pain Res
Spinal Cord Stimulation Alleviates Sensitization of Neuropathic Pain by Upregulating G Protein-Coupled Receptors to Inhibit Overexpression of Cav2.2 and Its Downstream Excitatory Neurotransmitters. [Abstract]2025 Jun 5:18:2775-2790. PMID: 40496674 -
Oncol Lett
JTC-801 inhibits the proliferation and metastasis of the Hep G2 hepatoblastoma cell line by regulating the phosphatidylinositol 3-kinase/protein kinase B signalling pathway. [Abstract]2019 Feb;17(2):1939-1945. PMID: 30675258
JTC-801 free base purchased from MedChemExpress. Usage Cited in: Oncol Lett. 2019 Feb;17(2):1939-1945. [Abstract]
Western blot analysis of proteins from Hep G2 cells treated with JTC‑801 for 24 h. The band intensities are quantified.
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J Recept Signal Transduct Res
JTC-801 exerts anti-proliferative effects in human osteosarcoma cells by inducing apoptosis. [Abstract]2018 Apr;38(2):133-140. PMID: 29447541
JTC-801 free base purchased from MedChemExpress. Usage Cited in: J Recept Signal Transduct Res. 2018 Apr;38(2):133-140. [Abstract]
JTC-801 down-regulates BCL-2 expression, and up-regulates BAX, Caspase-3 expression in U2OS cells.
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Pharmazie
JTC-801 inhibits the proliferation and metastasis of ovarian cancer cell SKOV3 through inhibition of the PI3K - AKT signaling pathway. [Abstract]2018 May 1;73(5):283-287. PMID: 29724295
JTC-801 free base purchased from MedChemExpress. Usage Cited in: Pharmazie. 2018 May 1;73(5):283-287. [Abstract]
Expression levels of proteins (BCL2, BAX and Active Caspase3) involved in the apoptotic pathway in the different SKOV3 groups, as detected by western blotting.
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Med Sci (Paris)
2018 Oct:34 Focus issue F1:8-14. PMID: 30403168
Purity & Documentation
References
[1]. Koyama T, et al. Nociceptin receptor antagonist JTC-801 inhibits nitrous oxide-induced analgesia in mice. J Anesth. 2009;23(2):301-3. [Content Brief]
[2]. Yamada H, et al. Pharmacological profiles of a novel opioid receptor-like1 (ORL(1)) receptor antagonist, JTC-801. Br J Pharmacol, 2002, 135(2), 323-332. [Content Brief]
[3]. Shinkai H, et al. 4-Aminoquinolines: novel nociceptin antagonists with analgesic activity. J Med Chem, 2000, 43(24), 4667-4677. [Content Brief]
[4]. Zhang Y, et al. Nociceptin/orphanin FQ peptide receptor antagonist JTC-801 reverses pain and anxiety symptoms in a rat model of post-traumatic stress disorder. Br J Pharmacol. 2015 Jan;172(2):571-82. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)