Molecular Weight(MW): 447.96
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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The effects of JTC-801, chloroquine phosphate, and SCF antibody on the expression of collagen type I in the dorsal skin of tranexamic acid-treated NOA mice. The values are expressed as the mean ± SD derived from 10 animals. *p < 0.05.
Antimicrob Agents Chemother, 2016, 60(6):3813-6. . JTC-801 purchased from Selleck.
The effects of JTC-801 and RU486 on the colitis score, body weight and length of the large intestine of the UVB/DSS-treated (A, B, C) andUVA/DSS-treated mice (D, E, F). The values represent the means±SD (C, F) and pooled SEM (A, B, D, E). *P < 0.05.
Photochem Photobiol, 2016, 92(5):728-34.. JTC-801 purchased from Selleck.
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Choose Selective Opioid Receptor Inhibitors
|Description||JTC-801 is a selective opioid receptor-like1 (ORL1) receptor antagonist with IC50 of 94 nM, weakly inhibits receptors δ, κ, and μ.|
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.  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. 
|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.  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.  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.  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).  JTC-801 produces dose-dependent mechanical and cold anti-allodynic effects with ED50 of 0.83 mg/kg and 1.02 mg/kg, respectively. |
-  Yamada H, et al. Br J Pharmacol, 2002, 135(2), 323-332.
-  Shinkai H, et al. J Med Chem, 2000, 43(24), 4667-4677.
-  Suyama H, et al. Neurosci Lett, 2003, 351(3), 133-136.
|In vitro||DMSO||90 mg/mL (200.91 mM)|
|Ethanol||31 mg/mL (69.2 mM)|
|In vivo||Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
For best results, use promptly after mixing.
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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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