SLIGRL-NH - CAS 171436-38-7
Category: Inhibitor
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Molecular Formula:
C29H56N10O7
Molecular Weight:
656.82
COA:
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Targets:
Protease-Activated Receptors (PARs)
Description:
LIGRL-NH2 is a PAR2 activator with EC50 value of ~5 µM. It can be used to explore signaling through PAR2 in cells.
Purity:
≥95% by HPLC
Synonyms:
L-Seryl-L-leucyl-L-isoleucylglycyl-L-arginyl-L-leucinamide; SL-NH2
MSDS:
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InChIKey:
SGPMJRPYYIJZPC-JYAZKYGWSA-N
InChI:
InChI=1S/C29H56N10O7/c1-7-17(6)23(39-27(45)21(12-16(4)5)38-25(43)18(30)14-40)28(46)35-13-22(41)36-19(9-8-10-34-29(32)33)26(44)37-20(24(31)42)11-15(2)3/h15-21,23,40H,7-14,30H2,1-6H3,(H2,31,42)(H,35,46)(H,36,41)(H,37,44)(H,38,43)(H,39,45)(H4,32,33,34)/t17-,18-,19-,20-,21-,23-/m0/s1
Canonical SMILES:
CCC(C)C(C(=O)NCC(=O)NC(CCCN=C(N)N)C(=O)NC(CC(C)C)C(=O)N)NC(=O)C(CC(C)C)NC(=O)C(CO)N
1.Long-term downregulation of protease-activated receptor-2 expression in distal colon in rats following bacillary dysentery.
Luo Y;Wang F;Qin J;Feng M;Lv Y;Wang Q;Liu K;Liu C Regul Pept. 2010 Aug 9;163(1-3):49-56. doi: 10.1016/j.regpep.2010.03.002. Epub 2010 Mar 27.
The aim of this study was to determine changes of PAR-2 expression in distal colon and the sensitivity of colonic muscle to SLIGRL-NH2, the PAR-2-activating peptide (PAR-2-AP) following bacillary dysentery. Shigella flexneri was administrated intragastrically in healthy male rats to induce bacillary dysentery. The effect of SLIGRL-NH2 on the motility of colonic muscle strips were examined. The expression of PAR-2 was determined by immunohistochemistry and Western blotting. Intragastric administration of S.flexneri induced acute inflammation at the mucosa of the distal colon at 4-11 days, and the inflammation disappeared 18 days later. PAR-2-AP-induced TTX insensitive relaxation of the colonic muscle strips. This inhibitory effect on colonic circular muscle strips was reduced on days 11-35, but the carbachol-induced contraction did not change. PAR-2 was located at the colon smooth muscles cells and myenteric nerve plexus. The amount of PAR-2 expression in distal colon was down regulated on days 11-35. These data indicated that bacillary dysentery exerted a long-term downregulation on the expression of PAR-2 in distal colon. This might be the reason of the low sensitivity of the colon circular muscle strips to the PAR-2-AP-induced relaxation following intragastric administration of S.
2.The spinal inhibition of N-type voltage-gated calcium channels selectively prevents scratching behavior in mice.
Maciel IS;Azevedo VM;Pereira TC;Bogo MR;Souza AH;Gomez MV;Campos MM Neuroscience. 2014 Sep 26;277:794-805. doi: 10.1016/j.neuroscience.2014.07.065. Epub 2014 Aug 7.
The present study investigated the effects of pharmacological spinal inhibition of voltage-gated calcium channels (VGCC) in mouse pruritus. The epidural administration of P/Q-type MVIIC or PhTx3.3, L-type verapamil, T-type NNC 55-0396 or R-type SNX-482 VGCC blockers failed to alter the scratching behavior caused by the proteinase-activated receptor 2 (PAR-2) activator trypsin, injected into the mouse nape skin. Otherwise, trypsin-elicited pruritus was markedly reduced by the spinal administration of preferential N-type VGCC inhibitors MVIIA and Phα1β. Time-course experiments revealed that Conus magus-derived toxin MVIIA displayed significant effects when dosed from 1h to 4h before trypsin, while the anti-pruritic effects of Phα1β from Phoneutria nigriventer remained significant for up to 12h. In addition to reducing trypsin-evoked itching, MVIIA or Phα1β also prevented the itching elicited by intradermal (i.d.) injection of SLIGRL-NH2, compound 48/80 or chloroquine, although they did not affect H2O2-induced scratching behavior. Furthermore, the co-administration of MVIIA or Phα1β markedly inhibited the pruritus caused by the spinal injection of gastrin-releasing peptide (GRP), but not morphine.
3.Lipopolysaccharide-induced subsensitivity of protease-activated receptor-2 in the mouse salivary glands in vivo.
Kawabata A;Kuroda R;Morimoto N;Kawao N;Masuko T;Kakehi K;Kataoka K;Taneda M;Nishikawa H;Araki H Naunyn Schmiedebergs Arch Pharmacol. 2001 Sep;364(3):281-4.
Protease-activated receptor-2 (PAR-2) acts as a modulator of multiple physiological/pathophysiological functions including salivary exocrine secretion. Given the supersensitivity of endothelial PAR-2 under endotoxaemia, we investigated if endotoxin/lipopolysaccharide (LPS) could alter the sensitivity of PAR-2 in the salivary glands. The in vivo salivation in response to i.v. administration of the PAR-2-activating peptide SLIGRL-NH2, but not of carbachol, gradually decreased 6-20 h after LPS administration in the mice. The LPS-induced hyporeactivity to the PAR-2 agonist was partially reversed by repeated administration of aprotinin, a non-specific protease inhibitor. PAR-2 mRNA levels in the salivary glands, as assessed by the semi-quantitative RT-PCR analysis, remained unchanged following LPS challenge. Our findings indicate that in contrast to the supersensitivity of endothelial PAR-2 as described previously, subsensitivity of PAR-2 in the salivary glands develops during the LPS-induced systemic inflammation, which might involve desensitisation of PAR-2 by endogenous proteases.
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Chemical Structure

CAS 171436-38-7 SLIGRL-NH

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