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F3681 Sigma

2-Furoyl-LIGRLO-amide trifluoroacetate salt

≥97% (HPLC)

Synonym: 2-Furoyl-Leu-Ile-Gly-Arg-Leu-Orn-NH2 trifluoroacetate salt, 2-Fly, 2-f-LIGRLO-NH2, 2-fAP, 2fLI, f-LIGRLO-NH2

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Properties

Related Categories Cell Biology, Cell Signaling and Neuroscience, Immune Cell Signaling and Blood, Immune System Regulation, Immunomodulators and Antibiotics More...
InChI Key   FPRULFHDSFKYBV-UHFFFAOYSA-N
assay   ≥97% (HPLC)
form   powder
color   white
storage temp.   −20°C

Description

Packaging

1 mg in glass bottle

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.

2-Furoyl-LIGRLO-amide trifluoroacetate salt is a highly potent agonist of proteinase-activated receptor-2 (PAR2). In KNRK cells with high number of PAR2 receptors, this agonist causes elevation of intracellular Ca2+ levels. Studies on rat show that it causes the relaxation of aorta rings in an endothelium-dependent manner.

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.

Price and Availability


All labs need water
Safety & Documentation

Safety Information

Symbol 
GHS07  GHS07
Signal word 
Warning
Hazard statements 
Precautionary statements 
Personal Protective Equipment 
RIDADR 
NONH for all modes of transport
WGK Germany 
3

Documents

Certificate of Analysis

Protocols & Articles
Peer-Reviewed Papers
15

References

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