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Protease-Activated Receptor-2, amide (SLIGKV-NH2)

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Protease-Activated Receptor-2, amide (SLIGKV-NH2)
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Cat #: V32060 CAS #: 190383-13-2 Purity ≥ 99%

Description: Protease-Activated Receptor-2, amide (peptide sequence shortening: SLIGKV-NH2), an activating peptide of PAR2, is a novel, highly potent and selective agonist of protease-activated receptor-2 (PAR2) (Ki = 9.64 μM; IC50 = 10.4 μM).

References: Kanke T, et al. Binding of a highly potent protease-activated receptor-2 (PAR2) activating peptide, [3H]2-furoyl-LIGRL-NH2, to human PAR2. Br J Pharmacol. 2005 May;145(2):255-63.

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Molecular Weight (MW)614.78
Molecular FormulaC28H54N8O7
CAS No.190383-13-2
ProtocolIn VitroThe PAR2-activating peptides used are: SLIGKV-OH, SLIGRL-OH, SLIGKV-NH2, SLIGRL-NH2. The synthetic agonist peptides mimicking the tethered ligand of PAR2, Ser-Leu-Ile-Gly-Lys-Val (SLIGKV-OH), Ser-Leu-Ile-Gly-Arg-Leu (SLIGRL-OH) and their amidated forms Ser-Leu-Ile-Gly-Lys-Val-amide (SLIGKV-NH2) Ser-Leu-Ile-Gly-Arg-Leu-amide (SLIGRL-NH2) have also been demonstrated being able to activate the receptor without enzymatic cleavage, therefore, have been utilised as biological tools to examine physiological functions of PAR2. Protease-Activated Receptor-2, amide is one of a four family subgroup of G-protein-coupled receptors (GPCRs), called PARs. Protease-activated receptors are distinguished from other GPCRs through their unique proteolytic mechanism of activation. For PAR2, activating proteases, such as trypsin, tryptase and coagulation factors VIIa and Xa, cleave a specific extracellular amino-terminal domain of the receptor to reveal a "tethered ligand", SLIGKV- and SLIGRL- for human and mouse/rat PAR2, respectively, which subsequently interacts with the activation domain of the receptor, initiating intracellular signaling pathways
These protocols are for reference only. InvivoChem does not independently validate these methods.
Preparing Stock Solutions
Solvent volume to be added Mass (the weight of a compound)
Mother liquor concentration 1mg5mg10mg20mg
1mM1.6266 mL8.1330 mL16.2660 mL32.5320 mL
5mM0.3253 mL1.6266 mL3.2532 mL6.5064 mL
10mM0.1627 mL0.8133 mL1.6266 mL3.2532 mL
20mM0.0813 mL0.4066 mL0.8133 mL1.6266 mL
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%DMSO + % + %Tween 80 + %ddH2O

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Method for preparing DMSO master liquid: mg drug pre-dissolved in µL DMSO(Master liquid concentration mg/mL) ,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation: Take µL DMSO master liquid, next add µL PEG300, mix and clarify, next add µL Tween 80,mix and clarify, next add µL ddH2O,mix and clarify.
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