Powder: -20°C for 3 years | In solvent: -80°C for 1 year
JTC-801 是一种选择性阿片受体样受体 1 (ORL1) 受体拮抗剂,Ki 值为 8.2 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
5 mg | ¥ 255 | 现货 | ||
10 mg | ¥ 417 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 421 | 现货 |
产品描述 | JTC-801 is a selective opioid receptor-like1 (ORL1) receptor antagonist with IC50 of 94 nM, weakly inhibits receptors δ, κ, and μ. |
靶点活性 | ORL1:94 nM |
体外活性 | 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] |
体内活性 | 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] |
激酶实验 | 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). |
别名 | JTC 801, N-(4-氨基-2-甲基-6-喹啉基)-2-[(4-乙基苯氧基)甲基]苯甲酰胺盐酸盐, JTC801 |
分子量 | 447.96 |
分子式 | C26H25N3O2·HCl |
CAS No. | 244218-51-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 44.8 mg/mL (100 mM)
Ethanol: 9 mg/mL (20 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / Ethanol | 1 mM | 2.2323 mL | 11.1617 mL | 22.3234 mL | 55.8086 mL |
5 mM | 0.4465 mL | 2.2323 mL | 4.4647 mL | 11.1617 mL | |
10 mM | 0.2232 mL | 1.1162 mL | 2.2323 mL | 5.5809 mL | |
20 mM | 0.1116 mL | 0.5581 mL | 1.1162 mL | 2.7904 mL | |
DMSO | 50 mM | 0.0446 mL | 0.2232 mL | 0.4465 mL | 1.1162 mL |
100 mM | 0.0223 mL | 0.1116 mL | 0.2232 mL | 0.5581 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
JTC-801 244218-51-7 Endocrinology/Hormones GPCR/G Protein Neuroscience Opioid Receptor Inhibitor inhibit JTC 801 N-(4-氨基-2-甲基-6-喹啉基)-2-[(4-乙基苯氧基)甲基]苯甲酰胺盐酸盐 JTC801 inhibitor