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.

• Sinônimo(s): PAR-2 Agonist I, Proteinase Activated Receptor-2 Agonist I, 2f-LIGRL-amide
• Fórmula empírica (Notação de Hill): C₃₁H₅₃N₉O₇
• Peso molecular: 663.81
• Código UNSPSC: 12352200
• NACRES: NA.77

Propriedades

• Nível de qualidade: 100
• Ensaio: ≥95% (HPLC)
• Formulário: lyophilized solid
• fabricante/nome comercial: Calbiochem^®
• condição de armazenamento: OK to freeze; desiccated (hygroscopic)
• cor: white
• solubilidade: DMSO: 5 mg/mL
• Condições de expedição: ambient
• temperatura de armazenamento: 2-8°C

Descrição

Descrição geral

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.

Ações bioquímicas/fisiológicas

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

Embalagem

Packaged under inert gas

Advertência

Toxicity: Standard Handling (A)

Sequência

2-Furoyl-Leu-Ile-Gly-Arg-Leu-NH₂

forma física

Supplied as a trifluoroacetate salt.

Reconstituição

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

Outras notas

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.

Informações legais

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

Informações de segurança

• Código de classe de armazenamento: 11 - Combustible Solids
• Classe de risco de água (WGK): WGK 1
• Ponto de fulgor (°F): Not applicable
• Ponto de fulgor (°C): Not applicable