JTC-801 free base

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JTC-801 free base is a selective opioid receptor-like1 (ORL1) receptor antagonist, binding to ORL1 receptor with a K_i value of 8.2?nM.

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

JTC-801 free base Chemical Structure

CAS No. : 244218-93-7

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Other In-stock Forms of JTC-801 free base:

JTC-801

Other Forms of JTC-801 free base:

JTC-801 In-stock

5 Publications Citing Use of MCE JTC-801 free base

: 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.

: 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.

: 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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μ Opioid Receptor/MOR κ Opioid Receptor/KOR δ Opioid Receptor/DOR NOP Receptor/ORL1

Biological Activity
Purity & Documentation
References
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Description

JTC-801 free base is a selective opioid receptor-like1 (ORL1) receptor antagonist, binding to ORL1 receptor with a K_i value of 8.2?nM.

IC₅₀ & Target

Ki: 8.2?nM (ORL1)^[2]

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	IC₅₀	1507 nM Compound: JTC-801	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	[PMID: 21330016]
HEK293	IC₅₀	30 nM Compound: JTC-801	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	[PMID: 21330016]
HEK293	IC₅₀	7512 nM Compound: JTC-801	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	[PMID: 21330016]

Molecular Weight

411.50

Formula

C₂₆H₂₅N₃O₂

CAS No.

244218-93-7

SMILES

O=C(C1=CC=CC=C1COC2=CC=C(C=C2)CC)NC3=CC=C4N=C(C=C(C4=C3)N)C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation

Handling Instructions (2659 KB)

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]

JTC-801 free base Related Classifications

Neurological Disease

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Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

JTC-801244218-93-7JTC801JTC 801Opioid ReceptorInhibitorinhibitorinhibit

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