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CAS No.: 244218-51-7

JTC-801 Catalog No. CSN16622

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

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技术信息

生物活性

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].
参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.2324 mL
- 11.1618 mL
- 22.3236 mL
- 5 mM
- 0.4465 mL
- 2.2324 mL
- 4.4647 mL
- 10 mM
- 0.2232 mL
- 1.1162 mL
- 2.2324 mL

技术信息

CAS号

244218-51-7

储存条件

粉末: Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C26H26ClN3O2

运输

蓝冰

分子量

447.96

别名

溶解度

DMSO	180.0 mg/mL (401.8 mM)
Water	insoluble

动物实验配方

0.5% methylcellulose+water

30 mg/mL

suspension

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