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Jtc-801  ≥98%

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包装规格：1mg 5mg 10mg 25mg 50mg 100mg in glass bottle
溶解性：溶于DMSO
产品描述：基本信息 产品编号： J70002 产品名称： Jtc-801 CAS: 244218-51-7   储存条件 粉末 -20℃ 四年     分子式： C26H26ClN3O2 溶于液体 -80℃ 6个月 分子量： 448.00 -20℃ 1个月 化学名：  N-(4-amino-2-methylquinolin-6-yl)-2-((4-ethylphenoxy)methyl)benzamide hydrochloride Solubility (25°C)：   体外:   DMSO 90mg/mL (200.91mM) Ethanol 31mg/mL (69.2mM) Water Insoluble 体内(现配现用): 0.5% methylcellulose 30mg/mL ＜1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 2.2323mL 11.1617mL 22.3234mL 5mM 0.4465mL 2.2323mL 4.4647mL 10mM 0.2232mL 1.1162mL 2.2323mL 50mM 0.0446mL 0.2232mL 0.4465mL   生物活性 产品描述 JTC-801 是一种具有选择性的 opioid receptor-like1 (ORL1) receptor 抑制剂，其 Ki 值为 8.2nM。 靶点 Opioid receptor-like1 (ORL1)  94nM   体外研究 JTC-801 inhibits [3H]-nociceptin binding to ORL1 receptor expressed in HeLa cells with an IC50 value of 94±8.6nm at a [3H]-nociceptin concentration of 50pM.JTC-801 weakly inhibits the binding of the ligands to human δ receptor (IC50>10μM),κ receptor (IC50>10μM),and μ receptor (IC50=325nM).In rat cerebrocortical membrane,JTC-801 inhibits ORL1 receptor (IC50=472nM) and μ receptor (IC50=1831nM).JTC-801 at a concentration of 10μM reverses the inhibitory action of nociceptin against forskolin-induced increase in cyclic AMP level (IC50:2.58μM,1nM of nociceptin used).JTC-801 alone does not affect the the production of cyclic AMP.The affinity of JTC-801 for ORL1 receptor,human opioid μ-,κ-,and δ-receptors is 8.2nM,102.9nM,1057.5nM and 8647.2nM. 体内研究 JTC-801 (≥0.01mg/kg,i.v. or 1mg/kg,p.o.) antagonizes the nociceptin-induced allodynia in mice.In mouse hot-plate test,JTC-801 prolongs escape response latency (ERL) to exposed heat stimulus with minimum effective doses (MED) of 0.01mg/kg by i.v.or 1mg/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 0.01mg/kg by i.v.administration or 1mg/kg by p.o.administration.This anti-nociceptive action of JTC-801 is not inhibited by naloxone (10mg/kg,s.c.).JTC-801 antagonizes the ORL1 receptor response,and has efficacious and potent anti-nociceptive effects in acute pain animal models not only by intravenous injection but also oral administration.JTC-801 (0.3mg/kg) decreases allodynia induced by the intrathecal injection of nociceptin in mice.JTC801 (6mg/kg i.p.,once daily) reverses SPS-induced mechanical allodynia,thermal hyperalgesia,anxiety-like behaviour and hypocortisolism.JTC-801 treatment also reverses NOP receptor protein and mRNA up-regulation in amygdala and PAG.JTC801 blocks elevated N/OFQ levels in serum,CSF,PAG and hippocampus at day 21 of SPS.JTC-801 (0.05-5mg/kg,i.p.) supresses the the analgesic effect of N2O in 129Sv mice by the writhing test and tail flick test.   推荐实验方法(仅供参考) 激酶实验： A suspension of membranes from human μ-opioid receptor-expressing CHO-K1 cells in 50mM Tris-HCl buffer (pH 7.4) containing 5mM MgCl2 and 10% sucrose is incubated at room temperature for 2.5h with 0.33nM 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 10μM naloxone.Specific binding is calculated by subtracting nonspecific binding from the total binding.Data are the mean±SE (n=3).   动物实验:   The antagonistic effect of naloxone,a non-specific opioid antagonist,on the anti-nociceptive effect of JTC-801 and morphine is examined by formalin stimulation test.Limb licking response is induced by subcutaneous injection of 50μL of 5% formalin to the left hind limb of each rat.The first 5 min (from immediately after the injection of formalin) and the subsequent 15 min (15-30 min post-injection) are designated as the first and second phases,respectively.The limb licking time during each of the phases is measured and used as an indicator of pain.Fifteen min before the injection of formalin,naloxone (10mg/kg,dissolved in physiological saline) is given subcutaneously.Five min before the injection of formalin,JTC-801 and morphine are dissolved in 5% sorbitol and given into the tail vein at doses of 0.03 and 1.0mg/kg,respectively.JTC-801 (3.0mg/kg) and morphine (30mg/kg) are administered orally 60 min before the formalin injection.
保存条件：-20℃

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