LRGILS-NH - CAS 245329-01-5
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
C29H56N10O7
Molecular Weight:
656.83
COA:
Inquire
Targets:
Protease-Activated Receptors (PARs)
Description:
LRGILS-NH is a control peptide for SLIGRL-NH2, a protease-activated receptor-2 (PAR2) agonist that facilitates gastrointestinal transit in vivo.
Purity:
≥95% by HPLC
Synonyms:
L-leucyl-L-arginylglycyl-L-isoleucyl-L-leucyl-L-serinamide
MSDS:
Inquire
InChIKey:
HCUFWKYFOMBFPA-JYAZKYGWSA-N
InChI:
InChI=1S/C29H56N10O7/c1-7-17(6)23(28(46)37-20(12-16(4)5)27(45)38-21(14-40)24(31)42)39-22(41)13-35-26(44)19(9-8-10-34-29(32)33)36-25(43)18(30)11-15(2)3/h15-21,23,40H,7-14,30H2,1-6H3,(H2,31,42)(H,35,44)(H,36,43)(H,37,46)(H,38,45)(H,39,41)(H4,32,33,34)/t17-,18-,19-,20-,21-,23-/m0/s1
Canonical SMILES:
CCC(C)C(C(=O)NC(CC(C)C)C(=O)NC(CO)C(=O)N)NC(=O)CNC(=O)C(CCCN=C(N)N)NC(=O)C(CC(C)C)N
1.Modified proteinase-activated receptor-1 and -2 derived peptides inhibit proteinase-activated receptor-2 activation by trypsin.
Al-Ani B;Saifeddine M;Wijesuriya SJ;Hollenberg MD J Pharmacol Exp Ther. 2002 Feb;300(2):702-8.
Trypsin activates proteinase-activated receptor-2 (PAR(2)) by a mechanism that involves the release of a tethered receptor-activating sequence. We have identified two peptides, FSLLRY-NH(2) (FSY-NH(2)) and LSIGRL-NH(2) (LS-NH(2)) that block the ability of trypsin to activate PAR(2) either in PAR(2)-expressing Kirsten virus-transformed kidney (KNRK) cell lines or in a rat aorta ring preparation. The reverse PAR(2) peptide, LRGILS-NH(2) (LRG-NH(2)) did not do so and FSY-NH(2) failed to block thrombin activation of PAR(1) in the aorta ring or in PAR(1)-expressing human embryonic kidney cells. Half-maximal inhibition (IC(50)) by FSY-NH(2) and LS-NH(2) of the activation of PAR(2) by trypsin in a PAR(2) KNRK calcium-signaling assay was observed at about 50 and 200 microM, respectively. In contrast, the activation of PAR(2) by the PAR(2)-activating peptide, SLIGRL-NH(2) (SL-NH(2)) was not inhibited by FSY-NH(2), LS-NH(2), or LRG-NH(2). In a casein proteolysis assay, neither FSY-NH(2) nor LS-NH(2) inhibited the proteolytic action of trypsin on its substrate. In addition, FSY-NH(2) and LS-NH(2) were unable to prevent trypsin from hydrolyzing a 20-amino acid peptide, GPNSKGR/SLIGRLDTPYGGC representing the trypsin cleavage/activation site of rat PAR(2).
2.Protease-activated receptor-2 (PAR-2)-related peptides induce tear secretion in rats: involvement of PAR-2 and non-PAR-2 mechanisms.
Nishikawa H;Kawai K;Tanaka M;Ohtani H;Tanaka S;Kitagawa C;Nishida M;Abe T;Araki H;Kawabata A J Pharmacol Exp Ther. 2005 Jan;312(1):324-31. Epub 2004 Aug 26.
Protease-activated receptor-2 (PAR-2) plays an extensive role in the regulation of digestive exocrine secretion. The present study examined whether PAR-2-related peptides could modulate tear secretion in rats and analyzed the underlying mechanisms. SLIGRL-NH(2), a PAR-2-activating peptide (PAR-2-AP) derived from mouse/rat PAR-2, when administered i.v. in combination with amastatin, an aminopeptidase inhibitor, evoked tear secretion, whereas LRGILS-NH(2), a PAR-2-inactive reversed peptide, had no such effect. In contrast, LSIGRL-NH(2), a partially reversed peptide known to be inactive with PAR-2, caused tear secretion equivalent to the effect of SLIGRL-NH(2). SLIGKV-NH(2), a human-derived PAR-2-AP, also induced significant tear secretion though to a lesser extent, whereas neither VKGILS-NH(2), a reversed peptide, nor LSIGKV-NH(2), a partially reversed peptide, produced any secretion. In desensitization experiments, after the first dose of SLIGRL-NH(2), the second dose of SLIGRL-NH(2) produced no tear secretion, whereas the response to LSIGRL-NH(2) was only partially inhibited by preadministration of SLIGRL-NH(2). Preadministration of LSIGRL-NH(2) abolished the response to subsequently administered LSIGRL-NH(2) but not SLIGRL-NH(2).
3.Proteinase-activated receptor 2 (PAR(2)): development of a ligand-binding assay correlating with activation of PAR(2) by PAR(1)- and PAR(2)-derived peptide ligands.
Al-Ani B;Saifeddine M;Kawabata A;Renaux B;Mokashi S;Hollenberg MD J Pharmacol Exp Ther. 1999 Aug;290(2):753-60.
A cloned rat proteinase-activated receptor (PAR)(2)-expressing cell line (KNRK-rPAR(2)) was used to study the structure-activity relationships (elevated intracellular Ca(2+)) for a series of: 1) PAR(1)-derived receptor-activating ligands (PAR(1)-APs) [SFLLR (P5), SFLLR-NH(2) (P5-NH(2)), SFLLRNP (P7), SFLLRNP-NH(2) (P7-NH(2)), and TFLLR-NH(2) (TF-NH(2))] and 2) PAR(2)-derived-activating-peptides (PAR(2)-APs) [SLIGRL-NH(2) (SL-NH(2)), SLIGR-NH(2) (GR-NH(2)), and SLIGKV-NH(2) (KV-NH(2))]. The activities of the PAR-APs were compared with the PAR(2)-AP analog trans-cinnamoyl-Leu-Ile-Gly-Arg-Leu-Orn-NH(2) tc-NH(2)), which as a [(3)H]propionyl derivative ([(3)H]propionyl-tc-NH(2)) was used to develop a radioligand-binding assay for PAR(2). The relative potencies of the PAR-APs in the Ca(2+)-signaling assay were tc-NH(2) = SL-NH(2) > KV-NH(2) congruent with P5-NH(2) > GR-NH(2) > P7-NH(2) > P7 > P5 > TF-NH(2). The reverse sequence PAR-APs, LSIGRL-NH(2) (LS-NH(2)), LRGILS-NH(2) (LR-NH(2)), FSLLRY-NH(2) (FSY-NH(2)), and FSLLR-NH(2) (FS-NH(2)), as well as the Xenopus PAR(1)-AP TFRIFD-NH(2), were inactive. The relative biological potencies of the peptides were in accord with their ability to compete for the binding of [(3)H]propionyl-tc-NH(2) (tc-NH(2) = SL-NH(2) > GR-NH(2) congruent with P5-NH(2) > P5) to KNRK-rPAR(2) cells, whereas inactive peptides (FS-NH(2); LR-NH(2)) showed no appreciable binding competition.
Molecular Weight Calculator Molarity Calculator Solution Dilution Calculator

Related Protease-Activated Receptors (PARs) Products


CAS 942413-05-0 VKGILS-NH2

VKGILS-NH2
(CAS: 942413-05-0)

VKGILS-NH2 is a reversed control peptide for SLIGKV-NH2, which is a protease-activated receptor 2 (PAR2) agonist.

CAS 1051487-82-1 AC 264613

AC 264613
(CAS: 1051487-82-1)

AC 264613 is a potent and selective protease-activated receptor 2 (PAR2) agonist (pEC50 = 7.5). AC 264613 inhibits interferon regulatory factor 5 and decreases ...

CAS 141136-83-6 Thrombin Receptor Activator Peptide 6

Thrombin Receptor Activator Peptide 6
(CAS: 141136-83-6)

TRAP-6, a peptide compound, has been found to be a PAR1 agonist and could also influence the phosphorylation of rapid phosphodiesterase 3A in the positive way.

CAS 729589-58-6 2-Furoyl-LIGRLO-amide

2-Furoyl-LIGRLO-amide
(CAS: 729589-58-6)

2-Furoyl-LIGRLO-amide is a potent and selective PAR2 receptor agonist (pD2 = 7.0). It causes a dose-dependent relaxation of murine femoral arteries.

BMS-986141

BMS-986141 is a dual antagonist of proteinase-activated receptor 1 (PAR1) and PAR4. BMS-986141 was confirmed in cynomolgus monkeys to be a better therapy for pr...

UDM-002555

UDM-002555 is a small-molecule and selective antagonist of protease-activated receptor-4 (PAR-4). It can suppress the activation of platelet in dose manner. In ...

Atopaxar
(CAS: 751475-53-3)

Atopaxar is a Protease-activated receptor-1 (PAR-1) inhibitor. It can inhibit the binding of a high-affinity thrombin receptor-activating peptide ([(3)H]haTRAP)...

CAS 171436-38-7 SLIGRL-NH

SLIGRL-NH
(CAS: 171436-38-7)

LIGRL-NH2 is a PAR2 activator with EC50 value of ~5 µM. It can be used to explore signaling through PAR2 in cells.

CAS 916170-19-9 AC-55541

AC-55541
(CAS: 916170-19-9)

AC-55541 is a novel small-molecule protease-activated receptor 2(PAR2) agonist which displays no activity at other PAR subtypes or at over 30 other receptors in...

CAS 245329-02-6 FSLLRY-NH2

FSLLRY-NH2
(CAS: 245329-02-6)

FSLLRY-NH2 is a selective PAR2 peptide antagonist. It reverses taxol-induced mechanical allodynia, heat hyperalgesia and PKC activation in ICR mice, also suppre...

CAS 474550-69-1 E 5555 hydrobromide

E 5555 hydrobromide
(CAS: 474550-69-1)

E 5555 hydrobromide is a potent and orally bioactive thrombin receptor (or protease-activated receptor 1, PAR1) antagonist (IC50 = 19 nM). It inhibits human pla...

CAS 173904-50-2 FR 171113

FR 171113
(CAS: 173904-50-2)

FR 171113 is a protease-activated receptor 1 (PAR1) antagonist displaying significant antiplatelet activity in vitro. It inhibits thrombin TRAP-6-induced platel...

CAS 89159-60-4 ML 354

ML 354
(CAS: 89159-60-4)

ML 354 is a selective PAR4 antagonist with IC50 value of 140 nM.

CAS 1216720-69-2 SCH 79797 dihydrochloride

SCH 79797 dihydrochloride
(CAS: 1216720-69-2)

SCH 79797 dihydrochloride is a potent and selective non-peptide PAR1 receptor antagonist (IC50 = 70 nM). SCH 79797 blocks haTRAP-induced human platelet aggregat...

CAS 190383-13-2 SLIGKV-NH2

SLIGKV-NH2
(CAS: 190383-13-2)

SLIGKV-NH2 is a protease-activated receptor 2 (PAR2) agonist (Ki = 9.64 μM; IC50 = 10.4 μM).

CAS 1252806-86-2 GB 83

GB 83
(CAS: 1252806-86-2)

GB 83 is a selective antagonist of human protease activated receptor 2 (PAR2) (IC50 = 2 mM).

CAS 327177-34-4 tcY-NH2

tcY-NH2
(CAS: 327177-34-4)

tcY-NH2 is a selective PAR4 antagonist peptide that inhibits aggregation caused by receptor-activating peptide analogs (GY-NH2, AY-NH2) and thrombin.

BMS-986120
(CAS: 1478712-37-6)

BMS-986120, an imidazoles derivative, has been found to be a PAR4 antagonist that could probably be effective against thrombus propagation and pathological vasc...

CAS 618385-01-6 Vorapaxar

Vorapaxar
(CAS: 618385-01-6)

SCH-530348 is a novel antiplatelet agent undergoing development by Schering-Plough Corp for the treatment and prevention of atherothrombosis. It is currently un...

CAS 245329-01-5 LRGILS-NH

LRGILS-NH
(CAS: 245329-01-5)

LRGILS-NH is a control peptide for SLIGRL-NH2, a protease-activated receptor-2 (PAR2) agonist that facilitates gastrointestinal transit in vivo.

Chemical Structure

CAS 245329-01-5 LRGILS-NH

Quick Inquiry

Verification code

Featured Items