2-(2-FUROYL)-LEU-ILE-GLY-ARG-LEU-ORN-NH2
Synonym(s):2-fAP;2fLI;2-f-LIGRLO-NH2;2-Fly;2-Furoyl-Leu-Ile-Gly-Arg-Leu-Orn-NH2 trifluoroacetate salt
- CAS NO.:729589-58-6
- Empirical Formula: C36H63N11O8
- Molecular Weight: 777.95
- MDL number: MFCD08460329
- SAFETY DATA SHEET (SDS)
- Update Date: 2023-06-30 15:45:59
What is 2-(2-FUROYL)-LEU-ILE-GLY-ARG-LEU-ORN-NH2?
The Uses of 2-(2-FUROYL)-LEU-ILE-GLY-ARG-LEU-ORN-NH2
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.
What are the applications of Application
2-Furoyl-LIGRLO-amide trifluoroacetate salt is a potent, selective PAR2 agonist
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
Properties of 2-(2-FUROYL)-LEU-ILE-GLY-ARG-LEU-ORN-NH2
Density | 1.33±0.1 g/cm3(Predicted) |
storage temp. | -20°C |
solubility | Soluble in H2O |
pka | 12.91±0.46(Predicted) |
form | powder |
color | white |
Water Solubility | Soluble to 1 mg/ml in water |
Safety information for 2-(2-FUROYL)-LEU-ILE-GLY-ARG-LEU-ORN-NH2
Signal word | Warning |
Pictogram(s) |
Exclamation Mark Irritant GHS07 |
GHS Hazard Statements |
H315:Skin corrosion/irritation H319:Serious eye damage/eye irritation H335:Specific target organ toxicity, single exposure;Respiratory tract irritation |
Precautionary Statement Codes |
P261:Avoid breathing dust/fume/gas/mist/vapours/spray. P264:Wash hands thoroughly after handling. P264:Wash skin thouroughly after handling. P271:Use only outdoors or in a well-ventilated area. P280:Wear protective gloves/protective clothing/eye protection/face protection. P302+P352:IF ON SKIN: wash with plenty of soap and water. P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing. |
Computed Descriptors for 2-(2-FUROYL)-LEU-ILE-GLY-ARG-LEU-ORN-NH2
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