CAS 190383-13-2|SLIGKV-NH2
| Common Name | SLIGKV-NH2 | ||
|---|---|---|---|
| CAS Number | 190383-13-2 | Molecular Weight | 614.77800 |
| Density | / | Boiling Point | / |
| Molecular Formula | C28H54N8O7 | Melting Point | / |
| MSDS | ChineseUSA | Flash Point | / |
Names
| Name | Ser-Leu-Ile-Gly-Lys-Val-amide |
|---|---|
| Synonym | More Synonyms |
SLIGKV-NH2 BiologicalActivity
| Description | Protease-Activated Receptor-2, amide (SLIGKV-NH2) is a highly potent protease-activated receptor-2 (PAR2) activating peptide. |
|---|---|
| Related Catalog | Signaling Pathways >>GPCR/G Protein >>Protease-Activated Receptor (PAR)Research Areas >>CancerPeptides |
| Target | PAR2[1] |
| In Vitro | The 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[1]. The protease-activated receptor-2 (PAR2) has been implicated in the pathogenesis of several inflammatory and autoimmune disorders, and is expressed in a wide variety of human tissues and cells. PAR2 belongs to a family of seven transmembrane domain receptor proteins that are activated by proteolysis. Enzymatic digestion exposes an N-terminus ligand sequence that binds intramolecularly to the activation site on the extracellular loop II, initiating a G-protein-mediated cell-signalling cascade and nuclear factor-kappa B (NF-κB)-regulated gene transcription[2]. |
| References | [1]. 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. [2]. Ramelli G, et al. Protease-activated receptor 2 signalling promotes dendritic cell antigen transport and T-cellactivation in vivo. Immunology. 2010 Jan;129(1):20-7. |
Chemical & Physical Properties
| Molecular Formula | C28H54N8O7 |
|---|---|
| Molecular Weight | 614.77800 |
| Exact Mass | 614.41200 |
| PSA | 260.86000 |
| LogP | 1.77930 |
| Appearance of Characters | solid |
| InChIKey | HOWDUIVVWDUEED-WAUHAFJUSA-N |
| SMILES | CCC(C)C(NC(=O)C(CC(C)C)NC(=O)C(N)CO)C(=O)NCC(=O)NC(CCCCN)C(=O)NC(C(N)=O)C(C)C |
| Storage condition | −20°C |
Safety Information
| Personal Protective Equipment | Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter |
|---|---|
| Safety Phrases | S22-S24/25 |
| RIDADR | NONH for all modes of transport |
| WGK Germany | 3 |
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Synonyms
| PAR-2 (1-6) Human |
| (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 |
