| Identification | Back Directory | [Name]
2-(2-FUROYL)-LEU-ILE-GLY-ARG-LEU-ORN-NH2 | [CAS]
729589-58-6 | [Synonyms]
2fLI
2-Fly
f-LIGRLO-NH2
2-f-LIGRLO-NH2
2F-LIGRLO-AMIDE
PAR-2 AGONIST II
2-FUROYL-LIGRLO-AMIDE
2-(2-FUROYL)-LIGRLOAMIDE
2-FUROYL-LEU-ILE-GLY-ARG-LEU-ORN-NH2
2-(2-FUROYL)-LEU-ILE-GLY-ARG-LEU-ORN-NH2
PROTEINASE ACTIVATED RECEPTOR-2 AGONIST II
2-Furoyl-LIGRLO-amide trifluoroacetate salt
(2-Furoyl)-PAR-2 (2-6)-Orn amide (mouse, rat)
2-(2-FUROYL)-PAR-2 (2-6)-ORN AMIDE (MOUSE, RAT)
2-Furoyl-Leu-Ile-Gly-Arg-Leu-Orn-NH2 trifluoroacetate salt
N-(2-Furanylcarbonyl)-L-leucyl-L-isoleucylglycyl-L-arginyl-L-leucyl-L-ornithinamide
2-Furoyl-LIGRLO-NH2 Potent and Selective Protease-Activated Receptor 2 (PAR2) Agonist
L-Ornithinamide, N-(2-furanylcarbonyl)-L-leucyl-L-isoleucylglycyl-L-arginyl-L-leucyl- | [Molecular Formula]
C36H63N11O8 | [MDL Number]
MFCD08460329 | [MOL File]
729589-58-6.mol | [Molecular Weight]
777.95 |
| Chemical Properties | Back Directory | [density ]
1.33±0.1 g/cm3(Predicted) | [storage temp. ]
-20°C | [solubility ]
Soluble in H2O | [form ]
powder | [pka]
12.91±0.46(Predicted) | [color ]
white | [Water Solubility ]
Soluble to 1 mg/ml in water |
| Hazard Information | Back Directory | [Uses]
2-Furoyl-LIGRLO-amide trifluoroacetate salt may be used as a protease-activated receptor 2 (PAR2) agonist in endothelial progenitor cells (EPCs) and in transient receptor potential cation channel subfamily V member (TRPV4)-transfected HEK293t cells. | [General Description]
2-Furoyl-LIGRLO-amide trifluoroacetate salt is a peptide that acts as a proteinase-activated receptor-2 (PAR2) agonist, and contains a furoyl group addition at its N-terminal. | [Biological Activity]
potent and selective par2 receptor agonist (pd2 = 7.0). causes a dose-dependent relaxation of murine femoral arteries. | [Biochem/physiol Actions]
2-Furoyl-LIGRLO-amide is a potent and selective protease-activated receptor 2 (PAR2) agonist. PAR-2 activation is associated with increases in cAMP and intracellular Ca(2+). Immunoblot analysis revealed increases in phosphorylation of epidermal growth factor (EGF) receptor (EGFR) tyrosine kinase, Src, Pyk2, cRaf, and ERK1/2 in response to PAR-2 activation. 2-Furoyl-LIGRLO-amide is nearly 100-fold more potent than SLIGRL-NH2 (Cat. No. S9317). 2-Furoyl-LIGRLO-amide caused both an endothelium-dependent relaxation and an endothelium-independent contraction. It produced delayed (6 hours later) facilitation of capsaicin-evoked visceral nociception, an effect being much more potent than SLIGRL-NH2. Such effects were mimicked by i.col. trypsin. 2-f-LIGRL-NH2, coadministered repeatedly with caerulein six times in total, abolished the caerulein-evoked abdominal hyperalgesia/allodynia in WT, but not PAR2-KO, mice. Repeated doses of 2-f-LIGRL-NH2 moderately attenuated the severity of caerulein-induced pancreatitis in WT animals. It induced a similar dose-dependent increase in Ca2 levels in the presence and absence of b-arrestins. | [storage]
Store at -20°C |
|
|