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JTC-801

Catalog No. T6553 CAS 244218-51-7

Synonyms: JTC 801, JTC801

JTC-801 is a selective opioid receptor-like1 (ORL1) receptor antagonist with IC50 of 94 nM, weakly inhibits receptors δ, κ, and μ.

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JTC-801, CAS 244218-51-7

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5 mg	In stock	$ 41.00
10 mg	In stock	$ 66.00
25 mg	In stock	$ 144.00
1 mL * 10 mM (in DMSO)	In stock	$ 65.00

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Purity: 99.27%

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Description	JTC-801 is a selective opioid receptor-like1 (ORL1) receptor antagonist with IC50 of 94 nM, weakly inhibits receptors δ, κ, and μ.
Targets&IC50	ORL1:94 nM
In vitro	JTC-801 displays about 12.5-, 129-, and 1055-fold selectivity for ORL1 receptor (Ki = 8.2 nM) over μ-, κ-, and δ-opioid receptors, respectively. JTC-801 does not inhibit forskolin-stimulated cyclic AMP accumulation in human ORL1 receptor-expressing HeLa cells, but it prevents nociceptin-induced inhibition of cyclic AMP accumulation, indicating that JTC-801 possesses full antagonistic activity. [2] In rat cerebrocortical membrane, JTC-801 inhibits ORL1 receptor with IC50 of 472 nM and μ-receptor with IC50 of 1831 nM. JTC-801 completely antagonizes the suppression of nociceptin on forskolin-induced accumulation of cyclic AMP with IC50 of 2.58 μM in HeLa cells expressing ORL1 receptor. [1]
In vivo	Oral administration of JTC-801 (0.3-3 mg/kg) antagonizes nociceptin-induced allodynia in mice, and shows analgesic effect in a hot plate test using mice and in a formalin test using rats. [2] In mouse hot-plate test, JTC-801 prolongs escape response latency (ERL) or exposed heat stimulus with minimum effective doses (MED) of 0.01 mg/kg by i.v. or 1 mg/kg by p.o. In the rat formalin test, JTC-801 reduces both the first and second phases of the nociceptive response with MED of 0.01 mg/kg71 by i.v. or 1 mg/kg by p.o. [1] JTC-801 dose-dependently normalizes paw withdrawal latency (PWL). Although JTC-801 does not inhibit a chronic constriction injury (CCI)-induced decrease in bone mineral content (BMC) and bone mineral density (BMD), it inhibits an increase in the number of osteoclasts. [3] Tactile allodynia induced by L5/L6 spinal nerve ligation is reversed by both systemic (3-30 mg/kg) and spinal (22.5 and 45 pg) JTC-801 in a dose-dependent manner. Furthermore, systemic JTC-801 reduces Fos-like immunoreactivity in the dorsal horn of the spinal cord (laminae I/II). [4] JTC-801 produces dose-dependent mechanical and cold anti-allodynic effects with ED50 of 0.83 mg/kg and 1.02 mg/kg, respectively. [6]
Kinase Assay	A suspension of membranes from human μ-opioid receptor-expressing CHO-K1 cells in 50 mM Tris-HCl buffer (pH 7.4) containing 5 mM MgCl2 and 10% sucrose is incubated at room temperature for 2.5 h with 0.33 nM 3H-labeled diprenorphine and various concentrations of JTC-801. The membranes are collected by filtration using Whatman 934-AH, and radioactivity is counted with a TopCount A9912V scintillation counter. Nonspecific binding (6.4%) is determined with 10 μM naloxone. Specific binding is calculated by subtracting nonspecific binding from the total binding. Data are the mean±SE (n=3).

Synonyms	JTC 801, JTC801
Molecular Weight	447.96
Formula	C26H25N3O2·HCl
CAS No.	244218-51-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 44.8 mg/mL (100 mM)

Ethanol: 9 mg/mL (20 mM)

References and Literature

1. Yamada H, et al. Br J Pharmacol, 2002, 135(2), 323-332. 2. Shinkai H, et al. J Med Chem, 2000, 43(24), 4667-4677. 3. Suyama H, et al. Neurosci Lett, 2003, 351(3), 133-136. 4. Tamai H, et al. Eur J Pharmacol, 2005, 510(3), 223-228. 5. Rawls SM, et al. Neuropeptides, 2007, 41(4), 239-247. 6. 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.

Related compound libraries

This product is contained In the following compound libraries：

Drug Repurposing Compound Library Anti-Cancer Clinical Compound Library Inhibitor Library Anti-Cancer Drug Library Membrane Protein-targeted Compound Library Anti-Neurodegenerative Disease Compound Library GPCR Compound Library Anti-Parkinson's Disease Compound Library ReFRAME Related Library Bioactive Compounds Library Max

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Keywords

JTC-801 244218-51-7 Endocrinology/Hormones GPCR/G Protein Neuroscience Opioid Receptor Inhibitor inhibit JTC 801 JTC801 inhibitor

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