Antibodies
JTC-801
- 貨號 Cat. No.
- S2722
- 規格 Size
- 10mM/1mL~50mg
- 品牌 Brand
- Selleckchem
Description
JTC-801
Catalog No.S2722
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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Distributor Tel: +886-2-2827-1197jimmy@new.abscience.com.tw
Biological Activity
| Description | 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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| Targets | Opioid receptor-like1 (ORL1) | |||||
| IC50 | 94 nM [1] | |||||
| 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] | |||||
| Features | ||||||
Protocol(Only for Reference)
Kinase Assay:
| Human ORL1 receptor binding affinity | Human ORL1 receptor expressed in HeLa cells are harvested and homogenized in 50 mM Tris buffer (pH 7.4) containing 1 mM EDTA. After centrifugation for 30 minutes at 40,000×g, the pellets are resuspended in buffer containing 50 mM Tris, supplemented with 10 mM MgCl2 and 2 mM EGTA, and used as membrane preparations. 50 mM Tris (pH 7.4) supplemented with 2 mM EDTA and 0.1 mM (p-amidoinophenyl) methanesulphonyl fluoride hydrochloride containing 0.2% bovine serum albumin is used for the binding buffer. For saturation binding assay, the cell membrane preparations are incubated for 60 minutes at 24 °C with various concentrations of [3H]-nociceptin. Nonspecific binding is determined in the presence of 1 mM unlabelled nociceptin. For competitive assay, the cell membrane preparations (4.17 μg/well) are incubated for 60 minutes at 24 °C with 50 pM [3H]-nociceptin in the presence of various concentrations of JTC-801 (10 nM-10 μM). JTC-801 is dissolved in DMSO and diluted in binding buffer, and then added to the incubation mixture. Final concentration of vehicle is 1% DMSO in binding buffer. After incubation for 60 minutes, the membrane preparations are rapidly filtrated over Whatman GF/B glass filters which are pretreated with 0.1% polyethyleneimine, and the radioactivity on each filter is measured by liquid scintillation counting. IC50 value is calculated as the concentration of JTC-801 required to displace 50% inhibition of the [3H]-nociceptin. |
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Animal Study:
| Animal Models | Male ICR (CD-1) subjected to nociceptin-induced allodynia test or hot plate test, and Male SD rats subjected to formalin-induced paw-licking response |
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| Dosages | ~10 mg/kg |
| Administration | Orally or injected i.v. |
| Solubility | 0.5% methylcellulose, 30 mg/mL |
References
Chemical Information
| Molecular Weight (MW) | 447.96 |
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| Formula | C26H25N3O2.HCl |
| CAS No. | 244218-51-7 |
| Storage | 3 years -20℃Powder |
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| 6 months-80℃in DMSO | |
| Syonnyms | N/A |
| Solubility (25°C) * | In vitro | DMSO | 90 mg/mL (200 mM) |
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| Water | <1 mg/mL (<1 mM) | ||
| Ethanol | 31 mg/mL (69 mM) | ||
| In vivo | 0.5% methylcellulose, | 30 mg/mL | |
| * <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. | |||
| Chemical Name | N-(4-amino-2-methylquinolin-6-yl)-2-((4-ethylphenoxy)methyl)benzamide hydrochloride |
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Preparing Stock Solutions
| Stock Solution (1ml DMSO) | 1mM | 10mM | 20mM | 30mM |
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| Mass(mg) | 0.44796 | 4.4796 | 8.9592 | 13.4388 |
