| AMG 9810TRPV1 antagonist |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
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- Purity = 99.76%
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| Cas No. | 545395-94-6 | SDF | Download SDF |
| Synonyms | N/A | ||
| Chemical Name | (E)-3-(4-(tert-butyl)phenyl)-N-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)acrylamide | ||
| Canonical SMILES | CC(C)(C)C1=CC=C(/C=C/C(NC2=CC=C3C(OCCO3)=C2)=O)C=C1 | ||
| Formula | C21H23NO3 | M.Wt | 337.41 |
| Solubility | ≥33.7mg/mL in DMSO | Storage | Store at -20°C |
| Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
AMG 9810 is a vanilloid receptor 1 (VR1 or TRPV1) antagonist, with IC50 values for human TRPV1 of 24.5±15.7 nM, for rat TRPV1 of 85.6 ±39.4 nM as a competitive antagonist of capsaicin activation. To block protons, its IC50 values for rat TRPV1 is 294±192 nM, for human TRPV1 is 92.7±72.8 nM. To block heat, its IC50 value for rat TRPV1 is 21±17 nM, for human TRPV1 is 15.8±10.8 nM. It can also block endogenous ligands, such as N-arachidonyl dopamine, anandamide and oleoyldopamine [1].
TRPV1 is expressed by peripheral sensory neurons. It is a membrane-bound, nonselective cation channel [1].
In rat dorsal root ganglia neurons with the presence of endogenous TRPV1, 45Ca2+ uptake was induced by capsaicin in a dose-dependent manner, the EC90 value is 300 nM. In a Ca2+-dependent manner, capsaicin induces CGRP release through the activation of TRPV1. Capsaicin at 300 nM induced a greater level of CGRP release from cultured neurons into the media, compared with the basal level. Capsaicin-induced 45Ca2+ uptake and CGRP release was potently blocked by AMG 9810 with IC50 values of 9±6 nM and 6±3 nM, respectively. AMG 9810 alone up to 10 ?M had no effect on the basal 45Ca2+ uptake or CGRP release of exposed neurons [1].
In animals capsaicin induced eye wipes. Intraperitoneally, AMG 9810 at 3, 10, and 30 mg/kg, dose-dependently decrease this effect at 15 min. Treatment with AMG 9810 at 10 and 30 mg/kg, 30 min before capsaicin treatment, statistically significantly reduced the number of eye wipes. Only treatment with AMG 9810 at 30 mg/kg 60 min before capsaicin administration significantly reduced eye wipes. Vehicle did not affect capsaicin-evoked eye wipes [1].
Reference: [1]. Gavva NR, Tamir R, Qu Y, et al. AMG 9810 [(E)-3-(4-t-butylphenyl)-N-(2, 3-dihydrobenzo[b][1,4] dioxin-6-yl)acrylamide], a novel vanilloid receptor 1 (TRPV1) antagonist with antihyperalgesic properties. J Pharmacol Exp Ther, 2005, 313(1):474-84.
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推荐了解“主细胞库”“工作细胞库”这两个名词。
① 在构建载体时，目的基因直接整合到细胞染色体组上，最好不要通过先瞬转在筛选稳定细胞株的这种方法，因为转染效率没有保证
② 高表达载体的构建，哺乳动物表达量一直是它自身的缺点，最好根据高表达载体定向的驯化细胞，提高蛋白表达量
③ 细胞的选择，筛选稳定细胞株我们常用的细胞是CHO，中国仓鼠卵巢细胞，由于CHO具有诸多的优点因此适合用于筛选稳定细胞株，而HEK293细胞则常用于瞬时转染
④ 后期的筛选，双抗预防污染，筛选细胞的时候抗生素浓度一定要做预实验，而且转染的时候不能有抗生素，关于细胞转染 稳定细胞系构建的相关理论
先提取RNA,反转录成cDNA,然后根据目的基因设计PCR引物,通过半定量RT-PCR确定目的基因表达.
正因为检测的是mRNA,所以要先反转录成cDNA才能PCR.
建立稳定细胞株,一般是根据不同基因载体中所含有的抗性标志选用相应的药物对靶...专注整体实验·服务生命科学已开展了数千个实验外包项目
