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Key Documents

SML0714

Sigma-Aldrich

FSLLRY-NH2 trifluoroacetate salt

≥98% (HPLC)

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About This Item

Formule empirique (notation de Hill):
C39H60N10O8 · xC2HF3O2
Numéro CAS:
245329-02-6
Poids moléculaire :
796.96 (free base basis)
Code UNSPSC :
12352200
Nomenclature NACRES :
NA.77

Niveau de qualité

100

Pureté

≥98% (HPLC)

Forme

powder

Couleur

white to off-white

Conditions d'expédition

wet ice

Température de stockage

−20°C

InChI

1S/C39H60N10O8/c1-22(2)17-30(36(55)45-28(11-8-16-44-39(42)43)35(54)46-29(33(41)52)20-25-12-14-26(51)15-13-25)47-37(56)31(18-23(3)4)48-38(57)32(21-50)49-34(53)27(40)19-24-9-6-5-7-10-24/h5-7,9-10,12-15,22-23,27-32,50-51H,8,11,16-21,40H2,1-4H3,(H2,41,52)(H,45,55)(H,46,54)(H,47,56)(H,48,57)(H,49,53)(H4,42,43,44)/t27-,28-,29-,30-,31-,32-/m0/s1

Clé InChI

KMSCNWHRNILNRJ-JNRWAQIZSA-N

Amino Acid Sequence

Phe-Ser-Leu-Leu-Arg-Tyr-NH2 trifluoroacetate salt

Application

FSLLRY-NH2 trifluoroacetate salt has been used as a protease-activated receptor 2 (PAR2) inhibitor to test its effects on urinary tract infections (UTIs) in a murine model. It has also been used to study the clinical itch datasets from phase 3 clinical trials for moderate-to-severe AD in atopic dermatitis (AD)-associated acute itch flare mice modelin rats.

Actions biochimiques/physiologiques

FSLLRY-NH2 is a peptide antagonist of the protease activated receptor 2 (PAR2). The peptide blocks agonist induced itching in rodent models. In cell based assays, the peptide inhibits agonist-induced cardiocyte remodeling, and production of cytokines by endothelial cells.
The ability of FSLLRY-NH2 to decrease visceral hypersensitivity (VH) suggests that PAR2 is involved in the maintenance of VH.

Code de la classe de stockage

11 - Combustible Solids

Classe de danger pour l'eau (WGK)

WGK 3

Point d'éclair (°F)

Not applicable

Point d'éclair (°C)

Not applicable

Certificats d'analyse (COA)

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Consulter la Bibliothèque de documents

Zonglong Wu et al.
American journal of physiology. Cell physiology, 317(3), C544-C555 (2019-06-27)
The specific regulatory mechanism of bladder urothelial barrier dysfunction after infection with uropathogenic Escherichia coli (UPEC) is still unclear. The cross talk between bladder urothelial cells and mast cells may play an important role during UPEC infection. In this study
Ying-Jie Li et al.
Digestive diseases and sciences, 64(5), 1182-1192 (2018-12-19)
Mast cells (MCs), PAR2 and TRPV1, play a key role in the regulation of visceral pain. Several studies have found that probiotics regulate visceral sensitivity. The purpose of the current study was to explore the role of MC-PAR2-TRPV1 in VH
Fang Wang et al.
Cell, 184(2), 422-440 (2021-01-16)
Itch is an evolutionarily conserved sensation that facilitates expulsion of pathogens and noxious stimuli from the skin. However, in organ failure, cancer, and chronic inflammatory disorders such as atopic dermatitis (AD), itch becomes chronic, intractable, and debilitating. In addition to

Articles

Proteinase-Activated Receptors

The search for a functional thrombin receptor, using expression cloning methods, led to the discovery of a G protein-coupled receptor that mediates the actions of thrombin on platelets and endothelial cells.

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