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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 Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 5 mg | Inquiry | 8-10 weeks | 8-10 weeks | |
| 50 mg | Inquiry | 8-10 weeks | 8-10 weeks |
| 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]. |
| Molecular Weight | 565.04 |
| Formula | C30H30ClFN4O4 |
| Cas No. | 2014368-93-3 |
| Smiles | C(C)(C)(C)C1=C2C(=NC(=C1)C3=CC(F)=C(Cl)C=C3)C=C(C(=O)N4C(C)(C)CN(CC4)C5=CC=C(C(O)=O)C=N5)O2 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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