AY-NH2
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.
AY-NH2是PAR4的选择性激动剂,EC50值为11 μM [1].
蛋白酶活化受体-4(PAR4)是PARs的成员,通过作用于G蛋白i\12/13(Rho和Ras活化)和q(钙信号),从而在介导凝血酶的细胞效应中起重要作用[2].
AY-NH2是高效的PAR4激动剂,比GYPGKF-NH2具有更高(约10倍)的活性.大鼠血小板凝集实验表明,AY-NH2比GY-NH2和GF-NH2具有更高的血小板凝集能力[1].野生型C57BL6小鼠分离出的富含血小板的血浆实验中,AY-NH2处理对PAR4表现出较高的激动活性,而对其它PARs没有作用[3].
在雄性Wistar大鼠足肿胀模型中,腹腔注射AY-NH2在响应毒性与非毒性机械刺激时能显著降低感受伤害评分,从而抑制角叉菜胶诱导的机械痛觉过敏和异常性疼痛[4].
参考文献:
[1]. Hollenberg, M.D., et al., Proteinase-activated receptor-4: evaluation of tethered ligandderived peptides as probes for receptor function and as inflammatory agonists in vivo. Br J Pharmacol, 2004. 143(4): p. 443-54.
[2]. Yu, G., et al., Increased expression of protease-activated receptor 4 and Trefoil factor 2 in human colorectal cancer. PLoS One, 2015. 10(4): p. e0122678.
[3]. Faruqi, T.R., et al., Structure-function analysis of protease-activated receptor 4 tethered ligand peptides. Determinants of specificity and utility in assays of receptor function. J Biol Chem, 2000. 275(26): p. 19728-34.
[4]. Asfaha, S., et al., Protease-activated receptor-4: a novel mechanism of inflammatory pain modulation. Br J Pharmacol, 2007. 150(2): p. 176-85.
Physical Appearance | White lyophilised solid |
Storage | Desiccate at -20°C |
M.Wt | 680.8 |
Cas No. | 352017-71-1 |
Formula | C34H48N8O7 |
Solubility | Soluble in H2O |
Chemical Name | (S,Z)-N-((Z)-2-(((S,Z)-6-amino-1-hydroxy-1-(((S)-1-hydroxy-1-imino-3-phenylpropan-2-yl)imino)hexan-2-yl)imino)-2-hydroxyethyl)-1-((S)-2-((Z)-((S)-2-amino-1-hydroxypropylidene)amino)-3-(4-hydroxyphenyl)propanoyl)pyrrolidine-2-carbimidic acid |
SDF | Download SDF |
Canonical SMILES | C[C@@](N)([H])/C(O)=N/[C@@](C(N1CCC[C@@]1([H])/C(O)=N/C/C(O)=N/[C@@](/C(O)=N/[C@@](C(O)=N)([H])CC2=CC=CC=C2)([H])CCCCN)=O)([H])CC3=CC=C(O)C=C3 |
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。 |