(±)-J 113397
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
(±)-J 113397是ORL1受体的强效选择性非肽类拮抗剂，对人类ORL1的Ki值为1.8 nM[1]。
ORL1受体是G蛋白偶联受体。它在结构上与阿片受体相关。十七肽痛敏肽/孤啡肽FQ是一种内源性配体[2]。
在CHO-ORL1细胞中，痛敏肽/孤啡剂量依赖性地抑制毛喉素诱发的cAMP的累积，EC50值为0.22 ± 0.011 nM。J-113397浓度增加引起痛敏肽/孤啡肽FQ浓度响应曲线右移。数据表明，J-113397以一种竞争方式抑制痛敏肽/孤啡肽与ORL1的相互作用[1]。
在甩尾试验中，小鼠侧脑室注射0.01-1 nmol的痛敏肽/孤啡肽FQ或生理盐水，生理盐水侧脑室注射没有明显改变甩尾的潜伏期。大于0.01-1 nmol的痛敏肽/孤啡肽FQ的剂量可缩短等待时间。使用J-113397注射15分钟后，痛敏肽/孤啡肽FQ作用达到最大跌幅。痛敏肽/孤啡肽FQ的作用持续了超过60分钟。J-113397会剂量依赖性地抑制痛敏肽/孤啡肽FQ诱导的小鼠甩尾潜伏期的缩短。30 mg/kg 剂量的J-113397可完全逆转痛敏肽/孤啡肽FQ引发的痛觉过敏[1]。
参考文献：
[1]. Ozaki S, Kawamoto H, Itoh Y, et al. In vitro and in vivo pharmacological characterization of J-113397, a potent and selective non-peptidyl ORL1 receptor antagonist. European journal of pharmacology, 2000, 402(1): 45-53.
[2]. Mollereau C, Mouledous L. Tissue distribution of the opioid receptor-like (ORL1) receptor. Peptides, 2000, 21(7): 907-917.
| Physical Appearance | White solid |
| Storage | Desiccate at RT |
| M.Wt | 399.57 |
| Cas No. | 217461-40-0 |
| Formula | C24H37N3O2 |
| Solubility | <19.98mg/ml in DMSO; <19.98mg/ml in ethanol |
| Chemical Name | 1-((3R,4R)-1-(cyclooctylmethyl)-3-(hydroxymethyl)piperidin-4-yl)-3-ethyl-1H-benzo[d]imidazol-2(3H)-one |
| SDF | Download SDF |
| Canonical SMILES | CCN(C1=O)C2=CC=CC=C2N1[C@]3([H])CCN(C[C@@]3([H])CO)CC4CCCCCCC4 |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
