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- 详细信息
- 文献和实验
- 技术资料
- 保存条件：
Powder: -20°C, 3 years; 4°C, 2 years. In solvent: -80°C, 6 months; -20°C, 1 month.
- 库存：
货期：1-2天
- 供应商：
MedChemExpress LLC
- CAS号：
545395-94-6
- 规格：
10 mM * 1 mL/1 mg/5 mg/10 mg/50 mg/100 mg
| 规格： | 10 mM * 1 mL | 产品价格： | ￥550.0 |
|---|---|---|---|
| 规格： | 1 mg | 产品价格： | ￥200.0 |
| 规格： | 5 mg | 产品价格： | ￥500.0 |
| 规格： | 10 mg | 产品价格： | ￥700.0 |
| 规格： | 50 mg | 产品价格： | ￥3000.0 |
| 规格： | 100 mg | 产品价格： | ￥5400.0 |
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AMG9810
CAS No. : 545395-94-6
MCE 国际站：AMG9810
产品活性：AMG9810是选择性和竞争性的香草素受体1 (TRPV1) 拮抗剂，对人类和大鼠TRPV1的IC50值分别为24.5 和 85.6 nM。
研究领域：Membrane Transporter/Ion Channel | Neuronal Signaling
作用靶点：TRP Channel
In Vitro: AMG9810 is a competitive antagonist of capsaicin activation (IC50 value for human TRPV1, 24.5±15.7 nM; rat TRPV1, 85.6±39.4 nM) and blocks all known modes of TRPV1 activation, including protons (IC50 value for rat TRPV1, 294±192 nM; human TRPV1, 92.7±72.8 nM), heat (IC50 value for rat TRPV1, 21±17 nM; human TRPV1, 15.8±10.8 nM), and endogenous ligands, such as anandamide, N-arachidonyl dopamine, and oleoyldopamine. AMG9810 blocks capsaicin-evoked depolarization and calcitonin gene-related peptide release in cultures of rat dorsal root ganglion primary neurons. AMG9810 inhibits capsaicin-, proton-, heat-, and endogenous ligand-induced uptake of 45Ca2+ into TRPV1-expressing cells.
In Vivo: AMG9810 is effective at preventing capsaicin-induced eye wiping in a dose-dependent manner, and it reverses thermal and mechanical hyperalgesia in a model of inflammatory pain induced by intraplantar injection of complete Freund's adjuvant. At effective doses, AMG9810 does not show any significant effects on motor function. AMG9810 is the first cinnamide TRPV1 antagonist reported to block capsaicin-induced eye wiping behavior and reverse hyperalgesia in an animal model of inflammatory pain. AMG9810, promotes mouse skin tumor development. The topical application of AMG9810 results in a significant increase in the expression level of the epidermal growth factor receptor (EGFR) and its downstream Akt/mammalian target of rapamycin (mTOR)-signaling pathway.
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文献和实验Silver Acetate Autometallography (AMG)
In the early eighties, a series of papers were published by Gorm DANSCHER, Aarhus, Denmark, to introduce a reliable and easy-to-handle technique for light microscopical and ultrastructural autometallographic (AMG) studies. Specific methods
王红阳院士等 Science 子刊报道老药新用的精准治疗机制，为 PTEN 突变肿瘤治疗带来新思路
）, 并将其用于药物筛选和分子谱分析，以寻找个性化的治疗方法和治疗机制。通过使用69种经过FDA批准的抗癌药库，对96孔板中培养的10个PDCs进行药物筛选测定，作者发现蛋白酶体抑制剂硼替佐米（bortezomib，多发性骨髓瘤治疗药物）对PDCs具有强大的细胞毒性作用。通过对胆管癌细胞系验证发现，不同细胞系对蛋白酶抑制剂的敏感性有所不同。 图片来源：Science Translational Medicine为了探究导致敏感性差异的机制，作者对两种代表性细胞系HCCC-9810（敏感）和RBE（不敏感）的进
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