PAR2 antagonist C391 | PAR2 antagonist | Probechem Biochemicals

Chemical Structure : PAR2 antagonist C391

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PAR2 antagonist C391 (Compound C391)

货号: PC-72283Not For Human Use, Lab Use Only.

PAR2 antagonist C391 (C391) is a selective PAR2 antagonist, potently inhibits peptidomimetic-induced PAR2 Ca2+ signalling with IC50 of 1.3 uM.

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生物&药学活性

PAR2 antagonist C391 (C391) is a selective PAR2 antagonist, potently inhibits peptidomimetic-induced PAR2 Ca2+ signalling with IC50 of 1.3 uM.
C391 blocks both PAR2 Ca2+ and MAPK signalling pathways activated by peptidomimetics and/or proteinase activation.
C391 effectively attenuated compound 48/80-induced thermal hyperalgesia in vivo.
C391 blocked A. alternata-induced, PAR2-dependent Ca2+ and MAPK signalling in 16HBE14o- cells, as well as β-arrestin recruitment in HEK 293 cells.
C391 effectively attenuated A. alternata-induced inflammation, mucus production, mucus cell hyperplasia and airway hyperresponsiveness in acute allergen-challenged murine models.

物理化学性质&存储条件

分子量	767.88
分子式	C38H53N7O10
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	((2S)-6-amino-2-((3S)-1-(furan-2-carbonyl)-3-(3-methylbutanamido)-4,7-dioxooctahydro-8H-pyrazino[1,2-a]pyrimidin-8-yl)hexanoyl)-L-leucyl-L-tyrosine

参考文献

1. Candy M Rivas, et al. Br J Pharmacol. 2021 Nov 28. doi: 10.1111/bph.15745.

2. Scott Boitano, et al. Br J Pharmacol. 2015 Sep;172(18):4535-4545.

3. Hassler SN, et al. Cephalalgia. 2019 Jan;39(1):111-122.

PAR2 antagonist C391 (Compound C391)

生物&药学活性

物理化学性质&存储条件

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PAR2 antagonist C391 (Compound C391)

生物&药学活性

物理化学性质&存储条件

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