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
Product does not compete with ATP.
Reversible: no
Packaging
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
Sequence
2-Furoyl-Leu-Ile-Gly-Arg-Leu-NH₂
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.
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.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Molecular Weight: 663.81. Empirical Formula: C31H53N9O7. Quality Level: 100. 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. Storage Class Code: 11 - Combustible Solids. WGK: WGK 1. Flash Point(F): Not applicable. Flash Point(C): Not applicable.- UPC:
- 51172445
- Condition:
- New
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- 539109-1MG