Shopping Cart
Remove All
  • TargetMol
    Your shopping cart is currently empty

I-287

Copy Product Info
😃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].

I-287

I-287

Copy Product Info
😃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
Add to Quotation
In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
Questions
TargetMol
View More

Resource Download

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
SmilesC(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 & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Calculator

  • Molarity Calculator
  • Dilution Calculator
  • Reconstitution Calculator
  • Molecular Weight Calculator

In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent 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.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent 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 ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
mg/kg
g
μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
Related Tags: buy I-287 | purchase I-287 | I-287 cost | order I-287 | I-287 chemical structure | I-287 in vivo | I-287 in vitro | I-287 formula | I-287 molecular weight