352017-71-1

Basic information

• Product Name: H-ALA-TYR-PRO-GLY-LYS-PHE-NH2
• Synonyms: PROTEASE-ACTIVATED RECEPTOR-4 AGONIST AMIDE;PAR-4 AGONIST AMIDE;H-ALA-TYR-PRO-GLY-LYS-PHE-NH2;AY-NH2;AYPGKFAMIDE;AYPGKF-NH2;(ALA1)-COAGULATION FACTOR II RECEPTOR-LIKE 3 (1-6) AMIDE (MOUSE);(ALA1)-PROTEINASE ACTIVATED RECEPTOR 4 (1-6) AMIDE (MOUSE)
• CAS NO: 352017-71-1
• Molecular Formula: C34H48N8O7
• Molecular Weight: 680.79
• Product Categories: Proteinase-activated receptor (PAR);Peptide Receptors;peptide
• Mol File: 352017-71-1.mol

Chemical Properties

• Boiling Point: 1143.1±65.0 °C(Predicted)
• Appearance: /solid
• Density: 1.285±0.06 g/cm3(Predicted)
• Storage Temp.: −20°C
• Solubility: Soluble in H2O
• PKA: 9.84±0.15(Predicted)
• Water Solubility: Soluble in water
• CAS DataBase Reference: H-ALA-TYR-PRO-GLY-LYS-PHE-NH2(CAS DataBase Reference)
• NIST Chemistry Reference: H-ALA-TYR-PRO-GLY-LYS-PHE-NH2(352017-71-1)
• EPA Substance Registry System: H-ALA-TYR-PRO-GLY-LYS-PHE-NH2(352017-71-1)

Safety Data

• Safety Statements: 22-24/25
• WGK Germany: 3
• Hazardous Substances Data: 352017-71-1(Hazardous Substances Data)

Usage

Uses

Used in Pharmaceutical Industry:
H-ALA-TYR-PRO-GLY-LYS-PHE-NH2 is used as a synthetic precursor for the preparation of PAR4 agonist peptides. These peptides are designed to activate the PAR4 receptor, which plays a crucial role in various physiological processes and has potential therapeutic applications in conditions such as thrombosis, inflammation, and cancer.
Used in Research Applications:
In the field of research, H-ALA-TYR-PRO-GLY-LYS-PHE-NH2 can be utilized as a building block for the development of novel peptides with specific biological activities. This peptide sequence can be incorporated into larger peptide structures or used as a starting point for the design of new molecules with targeted functions.
Used in Drug Development:
H-ALA-TYR-PRO-GLY-LYS-PHE-NH2 may also be employed in the development of new drugs, particularly those targeting the PAR4 receptor. By understanding the interactions between this peptide sequence and the receptor, researchers can design more effective and selective drug candidates for various therapeutic applications.

Biological Activity

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.