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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).
| Targets |
PAR2
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|---|---|
| ln Vitro |
The peptides that activate PAR2 are SLIGKV-OH, SLIGRL-OH, SLIGKV-NH2, and SLIGRL-NH2. Synthetic agonist peptides that mimic 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) Because Ser-Leu-Ile-Gly-Arg-Leu-amide (SLIGRL-NH2) has been shown to be able to activate the receptor without enzymatic cleavage, it has been used as a biological tool to investigate the physiological functions of PAR2. Among the four family subgroups of G-protein-coupled receptors (GPCRs), or PARs, is protease-activated receptor-2, amide. Protease-activated receptors are unique among GPCRs in that they are activated by a proteolytic mechanism. Trypsin, tryptase, and coagulation factors VIIa and Xa are examples of activating proteases for PAR2 that cleave a particular extracellular amino-terminal domain of the receptor to reveal a "tethered ligand," SLIGKV- for human PAR2 and SLIGRL- for mouse/rat PAR2, respectively. This ligand then interacts with the receptor's activation domain to start intracellular signaling pathways[1]. Protease-activated receptor-2 (PAR2) is expressed in a broad range of human tissues and cells and has been linked to the pathophysiology of multiple inflammatory and autoimmune disorders. Proteolysis activates a family of seven transmembrane domain receptor proteins, including PAR2. The process of enzymatic digestion reveals an N-terminus ligand sequence, which binds intramolecularly to the activation site on the extracellular loop II. This triggers nuclear factor-kappa B (NF-κB)-regulated gene transcription and a G-protein-mediated cell-signalling cascade[2].
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| References |
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| Molecular Formula |
C₂₈H₅₄N₈O₇
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|---|---|
| Molecular Weight |
614.78
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| Exact Mass |
614.41
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| CAS # |
190383-13-2
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| Sequence |
Ser-Leu-Ile-Gly-Lys-Val-NH2
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| Appearance |
White to off-white solid powder
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| SMILES |
CC[C@H](C)[C@@H](C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C(C)C)C(=O)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)N
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| InChi Key |
HOWDUIVVWDUEED-WAUHAFJUSA-N
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| InChi Code |
InChI=1S/C28H54N8O7/c1-7-17(6)23(36-27(42)20(12-15(2)3)34-25(40)18(30)14-37)28(43)32-13-21(38)33-19(10-8-9-11-29)26(41)35-22(16(4)5)24(31)39/h15-20,22-23,37H,7-14,29-30H2,1-6H3,(H2,31,39)(H,32,43)(H,33,38)(H,34,40)(H,35,41)(H,36,42)/t17-,18-,19-,20-,22-,23-/m0/s1
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| Chemical Name |
(2S)-6-amino-2-[[2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-amino-3-hydroxypropanoyl]amino]-4-methylpentanoyl]amino]-3-methylpentanoyl]amino]acetyl]amino]-N-[(2S)-1-amino-3-methyl-1-oxobutan-2-yl]hexanamide
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| Synonyms |
Ser-Leu-Ile-Gly-Lys-Val; PAR2 activating peptide; PAR2-AP; PAR-2 (1-6) Human; Protease-Activated Receptor-2, amide
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O: ~33.3 mg/mL (~54.2 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 100 mg/mL (162.66 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6266 mL | 8.1330 mL | 16.2660 mL | |
| 5 mM | 0.3253 mL | 1.6266 mL | 3.2532 mL | |
| 10 mM | 0.1627 mL | 0.8133 mL | 1.6266 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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