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Key Documents

SML0714

Sigma-Aldrich

FSLLRY-NH2 trifluoroacetate salt

≥98% (HPLC)

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About This Item

Fórmula empírica (notación de Hill):
C39H60N10O8 · xC2HF3O2
Número de CAS:
Peso molecular:
796.96 (free base basis)
UNSPSC Code:
12352200
NACRES:
NA.77

Quality Level

assay

≥98% (HPLC)

form

powder

color

white to off-white

shipped in

wet ice

storage temp.

−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

InChI key

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.

Biochem/physiol Actions

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.

Storage Class

11 - Combustible Solids

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable


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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
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
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

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