539109
PAR-2 Agonist I
The PAR-2 Agonist I controls the biological activity of PAR-2. This small molecule/inhibitor is primarily used for Activators/Inducers applications.
Synonym(s):
PAR-2 Agonist I, Proteinase Activated Receptor-2 Agonist I, 2f-LIGRL-amide
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About This Item
Empirical Formula (Hill Notation):
C31H53N9O7
Molecular Weight:
663.81
UNSPSC Code:
12352200
NACRES:
NA.77
Assay:
≥95% (HPLC)
Form:
lyophilized solid
Quality level:
Storage condition:
OK to freeze, desiccated (hygroscopic)
Quality Level
assay
≥95% (HPLC)
form
lyophilized solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, desiccated (hygroscopic)
color
white
solubility
DMSO: 5 mg/mL
shipped in
ambient
storage temp.
2-8°C
General description
Native proteinase activated receptor-2- (PAR-2) specific agonist, SLIGRL-NH2, modified with an N-terminal furoyl group to increase its potency and resistance to metabolic degradation. Shown to activate [Ca2+]i mobilization in PAR-2-expressing cells (EC50 = 253 nM in HCT-15 cells) in vitro. Also induces PAR-2-mediated salivation (ED50 = 30 nmol/kg, i.v.) in vivo. Exhibits no effects on PAR-2-/- mice. Reactive towards human, rat, and mouse PAR-2.
The native PAR-2-specific agonist, SLIGRL-NH2, is modified with an N-terminal furoyl group to increase its potency and resistance to metabolic degradation. Shown to activate [Ca2+]i mobilization in PAR-2-expressing cells (EC50 = 253 nM using HCT-15 cells) in vitro and induce PAR-2 mediated salivation (ED50 = 30 nmol/kg, i.v.) in vivo, while exhibiting no effect on PAR-2-/- mice. Reactive towards human, rat, and murine PAR-2.
Biochem/physiol Actions
Cell permeable: no
EC50 = 253 nM as PAR-2-specific agonist using HCT-15 cells
Primary Target
PAR-2
PAR-2
Product does not compete with ATP.
Reversible: no
Packaging
Packaged under inert gas
Physical form
Supplied as a trifluoroacetate salt.
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
2-Furoyl-Leu-Ile-Gly-Arg-Leu-NH₂
Kawabata, A., et al. 2004. J. Pharmacol. Exp. Ther.309, 108.
Kawabata, A., et al. 2004. J. Pharmacol. Exp. Ther.309, 1098.
Ferrell, W.R., et al. 2003. J. Clin. Invest.111, 35.
Kawabata, A., et al. 2004. J. Pharmacol. Exp. Ther.309, 1098.
Ferrell, W.R., et al. 2003. J. Clin. Invest.111, 35.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
Storage Class
11 - Combustible Solids
wgk
WGK 1
flash_point_f
Not applicable
flash_point_c
Not applicable
Certificates of Analysis (COA)
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