I-287 |CAS:2014368-93-3 Probechem Biochemicals

Chemical Structure : I-287

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I-287 (I 287)

货号: PC-38310Not For Human Use, Lab Use Only.

I-287 is a potent, selective, orally active inhibitor of PAR2, negative PAR2 allosteric modulator, inhibits PAR2-mediated activation of Gq and G12/13 but not Gi/o proteins (IC50=45-390 nM).

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生物&药学活性

I-287 is a potent, selective, orally active inhibitor of PAR2, negative PAR2 allosteric modulator, inhibits PAR2-mediated activation of Gq and G12/13 but not Gi/o proteins (IC50=45-390 nM).
I-287 is a negative allosteric modulator (NAM) and not an orthosteric competitive antagonist of hPAR2.
I-287 inhibits PAR2-mediated activation of DAG/Ca2+/PKC and RhoA/SRF-RE, as well as FAK and ERK1/2 signaling pathways, shows no effect on PAR2-mediated recruitment of βarrestin2 and receptor internalization.
I-287 inhibits PAR2-induced secretion of IL-8 cytokine in vitro and reduces Freund's adjuvant (CFA)-induced paw edema model in mice.

物理化学性质&存储条件

分子量	565.042
分子式	C30H30ClFN4O4
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	6-[4-[[5-(4-Chloro-3-fluorophenyl)-7-(1,1-dimethylethyl)furo[3,2-b]pyridin-2-yl]carbonyl]-3,3-dimethyl-1-piperazinyl]-3-pyridinecarboxylic acid

参考文献

1. Avet C, et al. Commun Biol. 2020 Nov 27;3(1):719.

I-287 (I 287)

生物&药学活性

物理化学性质&存储条件

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I-287 (I 287)

生物&药学活性

物理化学性质&存储条件

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