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.

• 別名: PAR-2 Agonist I, Proteinase Activated Receptor-2 Agonist I, 2f-LIGRL-amide
• 実験式（ヒル表記法）: C₃₁H₅₃N₉O₇
• 分子量: 663.81
• UNSPSCコード: 12352200
• NACRES: NA.77

特性

• 品質水準: 100
• アッセイ: ≥95% (HPLC)
• 形状: lyophilized solid
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze; desiccated (hygroscopic)
• 色: white
• 溶解性: DMSO: 5 mg/mL
• 輸送温度: ambient
• 保管温度: 2-8°C

詳細

詳細

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.

生物化学的／生理学的作用

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

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

シーケンス

2-Furoyl-Leu-Ile-Gly-Arg-Leu-NH₂

物理的形状

Supplied as a trifluoroacetate salt.

再構成

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

その他情報

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.

法的情報

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

安全性情報

• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 1
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable