Cas No.: | 352017-71-1 |
Chemical Name: | PAR-4 Agonist Peptide, amide |
Synonyms: | H-ALA-TYR-PRO-GLY-LYS-PHE-NH2;(Ala1)-PAR-4 (1-6) amide (mouse);AY-NH2;ALA-TYR-PRO-GLY-LYS-PHE-NH2;AYPGKFAMIDE;AYPGKF-NH2;PAR-4 AGONIST AMIDE;PROTEASE-ACTIVATED RECEPTOR-4 AGONIST AMIDE;Proteinase activated receptor 4 amide,mouse;PAR-4 Agonist Peptide, amide;PAR-4-AP;AY-NH2;352017-71-1;AKOS024456631;NCGC00485629-01;PAR-4-AP;H-Ala-Tyr-Pro-Gly-Lys-Phe-NH2;CS-0029355;(2S)-N-[2-[[(2S)-6-amino-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-1-oxohexan-2-yl]amino]-2-oxoethyl]-1-[(2S)-2-[[(2S)-2-aminopropanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]pyrrolidine-2-carboxamide;HY-P1309 |
SMILES: | C[C@H](N)C(N[C@H](C(N1CCC[C@H]1C(NCC(N[C@H](C(N[C@H](C(N)=O)CC2=CC=CC=C2)=O)CCCCN)=O)=O)=O)CC3=CC=C(O)C=C3)=O |
Formula: | C34H48N8O7 |
M.Wt: | 680.79432 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | AY-NH2 is a peptide agonist of proteinase-activated receptor 4 (PAR4) that induces aggregation of rat and human platelets in vitro (EC50s = 15 and 60 μM, respectively).It reduces expression of glycoprotein (GP) Ib, and increases expression of GPIIb/IIIa on the surface of human platelets.AY-NH2 induces relaxation of isolated rat aortic rings and contraction of rat gastric longitudinal muscle strips (EC50s = 11 and 110 μM, respectively) as well as inhibits calcium mobilization evoked by capsaicin in rat sensory neurons.In vivo, AY-NH2 (1-100 μg) increases latency to paw withdrawal and the nociceptive threshold in response to thermal and mechanical stimuli.AY-NH2 (200 μg) also increases paw thickness in a rat paw edema assay. |
Target: | PAR-4[1] |
In Vitro: | Compared with their BALB/cBy controls, SCID mice have a significantly greater abdominal response to colorectal distension (CRD) at the distension levels of 0.04 to 0.1 mL increasing the intensity of EMG response by 384% to 132%, respectively (P<0.01; P<0.01; P<0.01; P<0.001). PAR-4 activation effectively reverses this hypersensitivity (P<0.01, P<0.05; P<0.05; P<0.05) [1]. |
Animal Administration: | Mice[1] SCID mice Male SCID mice and their BALB/cBy controls are operated as C57BL/6J mice, and on the 4th postoperative day mice receive intracolonically (IC) infusion of 100 μg PAR-4-AP or vehicle. Visceral pain measurements started 1 h following the end of infusion[1]. |
References: | [1]. Annaházi A, et al. Proteinase-activated receptor-4 evoked colorectal analgesia in mice: an endogenously activatedfeed-back loop in visceral inflammatory pain. Neurogastroenterol Motil. 2012 Jan;24(1):76-85, e13. |