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I-191

Chemical Structure : I-191

CAS No.: 1690172-25-8

I-191 (I191)

Catalog No.: PC-62088Not For Human Use, Lab Use Only.

I-191 (I191, I 191) is a novel potent, selective protease-activated receptor 2 (PAR2) antagonist with pIC50 of 7.2 in cell-based assays.

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Biological Activity

I-191 is a novel potent, selective protease-activated receptor 2 (PAR2) antagonist with pIC50 of 7.2 in cell-based assays.
I-191 potently attenuates multiple PAR2-mediated intracellular signaling pathways leading to Ca2+ release, ERK1/2 phosphorylation, Ras homologue gene family, member A (RhoA) activation, and inhibition of forskolin-induced cAMP accumulation.
I-191 also potently inhibits PAR2-mediated downstream functional responses, including expression and secretion of inflammatory cytokines and cell apoptosis and migration, in human HT29 and MDA-MB-231 cells.

Physicochemical Properties

M.Wt 423.492
Formula C23H26FN5O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

4-(8-(tert-butyl)-6-(4-fluorophenyl)imidazo[1,2-b]pyridazine-2-carbonyl)-3,3-dimethylpiperazin-2-one

References

1. Jiang Y, et al. J Pharmacol Exp Ther. 2018 Feb;364(2):246-257.

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