JTC-801,NOP拮抗剂

98%

JTC-801

产品说明书 SDS 产品使用指南

品牌：源叶(MedMol)

产品编号：S80563 一键复制产品信息

CAS号：244218-51-7

分子式：C₂₆H₂₅N₃O₂·HCl

分子量：447.96

MDL：MFCD06198707

别名：N-(4-amino-2-methylquinolin-6-yl)-2-((4-ethylphenoxy)methyl)benzamide hydrochloride;JTC-801

货号	规格	价格	上海	北京	珠海	重庆	武汉
S80563-1mg促销	98%	￥226.00 ￥202.00 S80563-1mg ￥202.00 现货	10 10	-	-	-	-
S80563-5mg促销	98%	￥299.00 ￥269.00 S80563-5mg ￥269.00 现货	4 4	-	-	-	-
S80563-10mg促销	98%	￥449.00 ￥404.00 S80563-10mg ￥404.00 现货	5 5	-	-	-	-
S80563-50mg促销	98%	￥1340.00 ￥1210.00 S80563-50mg ￥1210.00 现货	2 2	-	-	-	-
S80563-100mg促销	98%	￥2110.00 ￥1900.00 S80563-100mg ￥1900.00 现货	2 2	-	-	-	-

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产品介绍参考文献质检证书(COA) 摩尔浓度计算器相关产品

产品描述：

JTC-801 is a selective opioid receptor-like1 (ORL1) receptor antagonist, binding to ORL1 receptor with a Ki value of 8.2 nM.

靶点：

Ki: 8.2 nM (ORL1);OpioidReceptor

体内研究：

JTC-801 (≥0.01 mg/kg, i.v. or 1 mg/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 0.01 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/kg by i.v. administration or 1 mg/kg by p.o. administration. This anti-nociceptive action of JTC-801 is not inhibited by naloxone (10 mg/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 (0.3 mg/kg) decreases allodynia induced by the intrathecal injection of nociceptin in mice. JTC-801 (6 mg/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. JTC-801 blocks elevated N/OFQ levels in serum, CSF, PAG and hippocampus at day 21 of SPS. JTC-801 (0.05-5 mg/kg, i.p.) supresses the the analgesic effect of N2O in 129Sv mice by the writhing test and tail flick test[

参考文献：

1. Yamada H, et al. Pharmacological profiles of a novel opioid receptor-like1 (ORL(1)) receptor antagonist, JTC-801. Br J Pharmacol, 2002, 135(2), 323-332. 2. Koyama T, et al. Nociceptin receptor antagonist JTC-801 inhibits nitrous oxide-induced analgesia in mice. J Anesth. 2009;23(2):301-3. 3. Shinkai H, et al. 4-Aminoquinolines: novel nociceptin antagonists with analgesic activity. J Med Chem, 2000, 43(24), 4667-4677. 4. Zhang Y, et al. Nociceptin/orphanin FQ peptide receptor antagonist JTC-801 reverses pain and anxiety symptoms in a rat model of post-traumatic stress disorder. Br J Pharmacol. 2015 Jan;172(2):571-82.

溶解性：

Soluble in DMSO、H2O

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.232 ml	11.162 ml	22.323 ml
5 mM	0.446 ml	2.232 ml	4.465 ml
10 mM	0.223 ml	1.116 ml	2.232 ml
50 mM	0.045 ml	0.223 ml	0.446 ml