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I-287

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Catalog No. T78672Cas No. 2014368-93-3

I-287 is a selective, orally active PAR2 inhibitor that functions as a negative allosteric modulator of Gαq and Gα12/13 activity and their downstream effectors. It has been shown to attenuate Complete Freund's adjuvant-induced inflammation in mice, suggesting its utility in inflammation/immunology research [1].

I-287

I-287

😃Good
Catalog No. T78672Cas No. 2014368-93-3
I-287 is a selective, orally active PAR2 inhibitor that functions as a negative allosteric modulator of Gαq and Gα12/13 activity and their downstream effectors. It has been shown to attenuate Complete Freund's adjuvant-induced inflammation in mice, suggesting its utility in inflammation/immunology research [1].
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
5 mgInquiry8-10 weeks8-10 weeks
50 mgInquiry8-10 weeks8-10 weeks
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Product Introduction

Bioactivity
Description
I-287 is a selective, orally active PAR2 inhibitor that functions as a negative allosteric modulator of Gαq and Gα12/13 activity and their downstream effectors. It has been shown to attenuate Complete Freund's adjuvant-induced inflammation in mice, suggesting its utility in inflammation/immunology research [1].
In vitro
I-287 (0-60 μM; 15-30 minutes) inhibits PAR2-mediated activation of Gαq and Gα12/13 proteins in HEK-293 cells without affecting Gi/o proteins and does not impact β-arrestin 2 recruitment or receptor internalization [1]. Additionally, I-287 (0-60 μM; 15-30 minutes) suppresses PAR2-mediated ERK1/2 activation [1]. At 10 μM for 30 minutes, I-287 also inhibits PAR2-induced IL-8 secretion in HCT-116 and A549 cells [1].
In vivo
I-287 (orally administered at a dosage of 50 mg/kg) reduced the inflammatory response induced by Complete Freund's adjuvant in C57BL/6J mice [1].
Chemical Properties
Molecular Weight565.04
FormulaC30H30ClFN4O4
Cas No.2014368-93-3
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

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