2-Furoyl-LIGRLO-amide trifluoroacetate salt
SIGMA/F3681 - ≥97% (HPLC)
Synonym: 2-Fly; 2-
CAS Number: 729589-58-6 (free base)
Empirical Formula (Hill Notation): C36H63N11O8 · xC2HF3O2
Molecular Weight: 777.95 (free base basis)
MDL Number: MFCD03821022
Linear Formula: C36H63N11O8 · xC2HF3O2
Product Type: Chemical
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| assay | ≥97% (HPLC) |
| color | white |
| form | lyophilized powder |
| InChI | 1S/C17H16ClN3OS/c1-9-7-10 |
| InChI key | FPRULFHDSFKYBV-UHFFFAOYSA |
| Quality Level | 100  |
| SMILES string | Cc1cc(C)c2c(N)c(sc2n1)C(= |
| storage temp. | −20°C |
| Application: | 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. |
| Biochem/physiol Actions: | 2-Furoyl-LIGRLO-amide is a potent and selective protease-activated receptor 2 (PAR2) agonist. |
| 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. |
| Biochem/physiol Actions: | 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. |
| Packaging: | 1 mg in glass bottle |
| Symbol |  GHS07 |
| Signal word | Warning |
| Hazard statements | H315 - H319 - H335 |
| Precautionary statements | P302 + P352 - P305 + P351 + P338 |
| Hazard Codes | Xi |
| Risk Statements | 36/37/38 |
| Safety Statements | 26 |
| RIDADR | NONH for all modes of transport |
| WGK Germany | WGK 3 |
| Flash Point(F) | Not applicable |
| Flash Point(C) | Not applicable |
| Purity | ≥97% (HPLC) |
| Storage Temp. | −20°C |
| UNSPSC | 51111800 |