AY-NH2
AY-NH2 is a selective agonist of PAR4 with EC50 value of 11 μM [1].
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) [2].
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 [1]. 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 [3].
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 [4].
References:
[1]. 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.
[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 |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
Quality Control & MSDS
- View current batch:
-
Purity ≥95.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
Chemical structure
