AY-NH2 is a selective agonist of PAR4 with EC50 value of 11 μM .
Protease-activated receptor-4 (PAR4) is a member of PARs and plays an important role in mediating cellular effects of thrombin through acting G-proteins i, 12/13 (Rho and Ras activation) and q (calcium signaling) .
AY-NH2 is a potent PAR4 agonist and has a higher (~10 fold) activity than GYPGKF-NH2. Using rat platelet aggregation assay, it was shown that AY-NH2 had highly platelet aggregation ability than GY-NH2 and GF-NH2 . When tested with platelet-rich plasma harvested from wild-type C57BL6 mice, AY-NH2 treatment exhibited highly agonist activity on PAR4 while had no effect on other PARs .
In male Wistar rats model of paw oedema, i.pl. injection of AY-NH2 markedly reduced the nociceptive score in response to both noxious and non-noxious mechanical stimuli, thus inhibiting carrageenan-induced mechanical hyperalgesia and allodynia .
. Hollenberg, M.D., et al., Proteinase-activated receptor-4: evaluation of tethered ligand-derived peptides as probes for receptor function and as inflammatory agonists in vivo. Br J Pharmacol, 2004. 143(4): p. 443-54.
. 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.
. 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.
. 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|
|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|
|Canonical SMILES||C[[email protected]@](N)([H])/C(O)=N/[[email protected]@](C(N1CCC[[email protected]@]1([H])/C(O)=N/C/C(O)=N/[[email protected]@](/C(O)=N/[[email protected]@](C(O)=N)([H])CC2=CC=CC=C2)([H])CCCCN)=O)([H])CC3=CC=C(O)C=C3|
|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.|