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.

• 别名: PAR-2 Agonist I, Proteinase Activated Receptor-2 Agonist I, 2f-LIGRL-amide
• 经验公式（希尔记法）: C₃₁H₅₃N₉O₇
• 分子量: 663.81
• UNSPSC代码: 12352200
• NACRES: NA.77

属性

• 质量水平: 100
• 方案: ≥95% (HPLC)
• 表单: lyophilized solid
• 制造商/商品名称: Calbiochem^®
• 储存条件: OK to freeze; desiccated (hygroscopic)
• 颜色: white
• 溶解性: DMSO: 5 mg/mL
• 运输: ambient
• 储存温度: 2-8°C

说明

一般描述

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.

生化/生理作用

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)

序列

2-Furoyl-Leu-Ile-Gly-Arg-Leu-NH₂

外形

Supplied as a trifluoroacetate salt.

重悬

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

其他说明

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.

法律信息

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

安全信息

• 储存分类代码: 11 - Combustible Solids
• WGK: WGK 1
• 闪点(°F): Not applicable
• 闪点(°C): Not applicable