AM679
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.
AM679是局部应用的和有效的5-脂氧合酶激活蛋白(FLAP)抑制剂,其IC50值为2.2 nM[1][2]。
FLAP和5-脂氧合酶(5-LO)共同将膜衍生花生四烯酸转换为促炎介质白三烯环氧化物LTA4。随后,LTA4在LTA4水解酶或LTC4合成酶作用下,对应地被迅速转换为LTB4或LTC4[2]。
与AM679共同孵育5小时,可以增强人血液对LTB4产生的抑制作用,其IC50值为53 nM。同样,与AM679共同孵育4小时,也可以时间依赖性地增强大鼠血液对LTB4产生的抑制作用,其IC50值为9 nM[2]。
半胱氨酰白三烯(CysLTs)被称为炎症和过敏的催化剂。感染RSV的小鼠眼睛于感染后的第4天开始出现眼部CysLTs浓度增加。在第6 ~ 8天眼部CysLTs浓度达峰期,AM679可以将其峰值降低90%以上。于第10天,经AM679处理的小鼠眼睛和对照组的CysLT浓度均几乎降至基线值。在人类过敏性结膜炎中,RSV和IL-4的mRNA间呈现出强相关性。在RSV感染后的第6天,IL-4的mRNA浓度在感染RSV的小鼠中呈现出显著的升高。在第14天左右,IL-4的mRNA浓度逐渐降至基线附近。对于由RSV感染引起的IL-4增加,AM679对其抑制作用高达80%以上[1]。
参考文献:
[1]. Alla Musiyenko, Lucia Correa, Nicholas Stock, et al. A Novel 5-Lipoxygenase-Activating Protein Inhibitor, AM679, Reduces Inflammation in the Respiratory Syncytial Virus-Infected Mouse Eye. Clinical and Vaccine Immunology, 2009, 16(11):1654-1659.
[2]. Nicholas Stock, Christopher Baccei, Gretchen Bain, et al. 5-Lipoxygenase-activating protein inhibitors. Part 2: 3-{5-((S)-1-Acetyl-2,3-dihydro-1H-indol-2-ylmethoxy)-3-tert-butylsulfanyl-1-[
4-(5-methoxy-pyrimidin-2-yl)-benzyl]-1H-indol-2-yl}-2,2-dimethyl-propionic acid (AM679)—A potent FLAP inhibitor. Bioorganic & Medicinal Chemistry Letters, 2010, 20:213-217.
Physical Appearance | A crystalline solid |
Storage | Store at -20°C |
M.Wt | 692.87 |
Cas No. | 1206880-66-1 |
Formula | C40H44N4O5S |
Synonyms | AM-679;AM 679 |
Solubility | Soluble in DMSO |
Chemical Name | 3-[5-[[(2S)-1-acetyl-2,3-dihydroindol-2-yl]methoxy]-3-tert-butylsulfanyl-1-[[4-(5-methoxypyrimidin-2-yl)phenyl]methyl]indol-2-yl]-2,2-dimethylpropanoic acid |
SDF | Download SDF |
Canonical SMILES | CC(=O)N1C(CC2=CC=CC=C21)COC3=CC4=C(C=C3)N(C(=C4SC(C)(C)C)CC(C)(C)C(=O)O)CC5=CC=C(C=C5)C6=NC=C(C=N6)OC |
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。 |
Description | AM679是5-脂氧合酶激活蛋白(FLAP)的选择性抑制剂。 | |||||
靶点 | FLAP | |||||
IC50 |