JTC-801

製品コードS2722 バッチS272201

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C26H25N3O2.HCl
分子量 447.96 CAS No. 244218-51-7
Solubility (25°C)* 体外 DMSO 90 mg/mL (200.91 mM)
Ethanol 31 mg/mL (69.2 mM)
Water Insoluble
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
0.5% methylcellulose
10.0mg/ml Taking the 1 mL working solution as an example, take 10 mg of this product, add it to 1 ml of 0.5% methylcellulose clear solution, and mix evenly to form a uniform suspension. The mixed solution should be used immediately for optimal results. 
* <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.

溶剤液（一定の濃度）を調合する

生物活性

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

プロトコル(参考用のみ)

キナーゼアッセイ 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.
動物実験 動物モデル 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
投薬量 ~10 mg/kg
投与方法 Orally or injected i.v.

カスタマーフィードバック

, , Antimicrob Agents Chemother, 2016, 60(6):3813-6.

Data from [Data independently produced by , , Photodermatol Photoimmunol Photomed, 2017, 33(2):84-91]

Data from [Data independently produced by , , Photochem Photobiol, 2016, 92(5):728-34.]

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長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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