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.

• 동의어(들): PAR-2 Agonist I, Proteinase Activated Receptor-2 Agonist I, 2f-LIGRL-amide
• 실험식(Hill 표기법): C₃₁H₅₃N₉O₇
• Molecular Weight: 663.81
• UNSPSC 코드: 12352200

속성

• Quality Level: 100
• 분석: ≥95% (HPLC)
• 형태: lyophilized solid
• 제조업체/상표: Calbiochem^®
• 저장 조건: OK to freeze; desiccated (hygroscopic)
• 색상: white
• solubility: DMSO: 5 mg/mL
• 배송 상태: ambient
• 저장 온도: 2-8°C

설명

일반 설명

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.

생화학적/생리학적 작용

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

포장

Packaged under inert gas

경고

Toxicity: Standard Handling (A)

서열

2-Furoyl-Leu-Ile-Gly-Arg-Leu-NH₂

물리적 형태

Supplied as a trifluoroacetate salt.

재구성

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

기타 정보

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.

법적 정보

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

안전성 정보

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 1
• Flash Point (°F): Not applicable
• Flash Point (°C): Not applicable