2-Furoyl-LIGRLO-amide trifluoroacetate salt

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2-Furoyl-LIGRLO-amide trifluoroacetate salt: sc-213814	\| Datasheet/SDS

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C₃₆H₆₃N₁₁O₈ • xC₂HF₃O₂, MW: 777.95 (free base basis), CAS: 729589-58-6 (free base)
1 mg
A potent, selective protease-activated receptor 2 (PAR2) agonist where 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, Pyk2, cRaf, Src and ERK1/2 in response to PAR-2 activation. This compound is nearly 100-fold more potent than SLIGRL-NH2. 2-Furoyl-LIGRLO-amide caused both an endothelium-dependent relaxation and an endothelium-independent contraction. Studies showed that 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.
Soluble in Water: >2 mg/mL
white
Gardell, L.R., et al., Identification and characterization of novel small molecule protease activated receptor 2 (PAR2) agonists. J. Pharmacol. Exp. Ther., (2008); Hollenberg, M.D., et al., Derivatized 2-furoyl-LIGRLO-amide, a versatile and selective probe for proteinase-activated receptor 2: binding and visualization. J. Pharmacol. Exp. Ther. 326, 453-462, (2008); Niu, Q.X., et al., Induction of inflammatory cytokine release from human umbilical vein endothelial cells by agonists of proteinase-activated receptor-2. Clin. Exp. Pharmacol. Physiol. 35, 89-96, (2008)
For Research Use Only

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Product Name	Catalog #	Unit	Price	Qty	Add
2-Furoyl-LIGRLO-amide trifluoroacetate salt	sc-213814	1 mg	$89

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2-Furoyl-LIGRLO-amide trifluoroacetate salt: sc-213814