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Merck

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.

Synonym(s):

PAR-2 Agonist I, Proteinase Activated Receptor-2 Agonist I, 2f-LIGRL-amide

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About This Item

Empirical Formula (Hill Notation):
C31H53N9O7
Molecular Weight:
663.81
UNSPSC Code:
12352200
NACRES:
NA.77

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Product Name

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.

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

Quality Level

100

Related Categories

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

Disclaimer

Toxicity: Standard Handling (A)

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.

Other Notes

2-Furoyl-Leu-Ile-Gly-Arg-Leu-NH₂
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.

Packaging

Packaged under inert gas

Physical form

Supplied as a trifluoroacetate salt.

Preparation Note

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

Legal Information

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

Storage Class

11 - Combustible Solids

wgk

WGK 1

flash_point_f

Not applicable

flash_point_c

Not applicable

Certificates of Analysis (COA)

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