PAR-2 Agonist I

Biochem/physiol Actions

Cell permeable: no

Reversible: no

Product does not compete with ATP.

EC50 = 253 nM as PAR-2-specific agonist using HCT-15 cells

Primary TargetPAR-2

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.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

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.

Packaging

1, 5 mg in Plastic ampoule

Packaged under inert gas

Physical form

Supplied as a trifluoroacetate salt.

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Sequence

2-Furoyl-Leu-Ile-Gly-Arg-Leu-NH₂

Warning

Toxicity: Standard Handling (A)