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JTC-801

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Chemical Structure| 244218-51-7 同义名 : -
CAS号 : 244218-51-7
货号 : A524466
分子式 : C26H26ClN3O2
纯度 : 98%
分子量 : 447.957
MDL号 : MFCD06198707
存储条件：

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(234.4 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

0.5% methylcellulose+water 30 mg/mL suspension

生物活性
靶点

  • ORL1

    Opioid receptor-like1 (ORL1), IC50:94 nM
描述 The nociceptin/orphanin FQ (N/OFQ)/N/OFQ receptor (NOP) system controls different biological functions including pain and cough reflex[3]. JTC-801 is a nociceptin/orphanin FQ opioid peptide (NOP) receptor antagonist, a single or multiple systemic administrations of JTC-801 significantly alleviated mechanical allodynia in paclitaxel-treated rats. Multiple injections of JTC-801 significantly inhibited the activation of Akt and decreased the expression of inflammatory cytokines [4]. The expression of anti-apoptotic protein B-cell lymphoma 2 decreased and the expression of the pro-apoptotic proteins active caspase-3 and apoptosis regulator BAX increased in the Hep G2 cells following JTC-801 treatment[5]. The JTC-801 significantly decreased the viability of U2OS cells (p < . 05) , its anti-proliferative effect through induction of apoptosis associated with activation of BAX, Caspase-3 and down-regulating BCL-2 expression. The invasive and migratory cells were obviously reduced after JTC-801 treatment (p < . 05). The phosphorylated AKT, mTOR and active p70 S6 protein kinase in the PI3K/AKT signaling pathway were obviously lessened in the JTC-801 treated U2OS group (p < . 05)[6]. 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[7].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.23mL

0.45mL

0.22mL

11.16mL

2.23mL

1.12mL

22.32mL

4.46mL

2.23mL
参考文献

[1]Yamada H, Nakamoto H, et al. Pharmacological profiles of a novel opioid receptor-like1 (ORL(1)) receptor antagonist, JTC-801. Br J Pharmacol. 2002 Jan;135(2):323-32.

[2]Shinkai H, Ito T, et al. 4-Aminoquinolines: novel nociceptin antagonists with analgesic activity. J Med Chem. 2000 Nov 30;43(24):4667-77.

[3] Salvatore Pacifico, Valentina Albanese,et al. Novel Mixed NOP/Opioid Receptor Peptide Agonists. J Med Chem. 2021 May 27;64(10):6656-6669.

[4] Jingxiu Huang, Dongtai Chen，et al. JTC-801 alleviates mechanical allodynia in paclitaxel-induced neuropathic pain through the PI3K/Akt pathway. Eur J Pharmacol. 2020 Sep 15;883:173306.

[5] Bufei Zhao, Ting Hu. JTC-801 inhibits the proliferation and metastasis of the Hep G2 hepatoblastoma cell line by regulating the phosphatidylinositol 3-kinase/protein kinase B signalling pathway. Oncol Lett. 2019 Feb;17(2):1939-1945.

[6] Chang-Jun Zheng, Li-Li Yang,et al. JTC-801 exerts anti-proliferative effects in human osteosarcoma cells by inducing apoptosis. J Recept Signal Transduct Res. 2018 Apr;38(2):133-140.

[7]Shinkai H, et al. 4-Aminoquinolines: novel nociceptin antagonists with analgesic activity. J Med Chem, 2000, 43(24), 4667-4677.