Cat. No.: HY-148016

I-287

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I-287 is a orally active selective PAR2 inhibitor that acting as a negative allosteric regulator on Gα_q and Gα_12/13 activity and their downstream effectors. I-287 reduces Complete Freund's adjuvant (HY-153808)-induced inflammation in mice and can be used for inflammation/immunology research.

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Pureté: 99.36%
CAS No.: 2014368-93-3
Formule: C₃₀H₃₀ClFN₄O₄
Masse moléculaire:565.04

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

I-287 Chemical Structure

CAS No.: 2014368-93-3

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Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target^[1]

PAR2

Voir tous les produits spécifiques à Isoform Protease Activated Receptor (PAR) :

Voir tous les produits spécifiques à Isoform ERK :

In Vitro

I-287 (0-60 μM; 15-30 min) inhibits PAR2-mediated activation of Gα_q and Gα_12/13 but not G_i/o proteins while has no effect on PAR2-mediated recruitment of βarrestin2 and receptor internalization^[1].
I-287 (0-60 μM; 15-30 min) inhibits PAR2-mediated ERK1/2 activation in HEK293 cells^[1].
I-287 (10 μM; 30 min) inhibits PAR2-induced secretion of IL-8 cytokine in HCT-116 and A549 cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis^[1]

Cell Line:

HEK-293 cells
Concentration:

0-60 μM
Incubation Time:

15 min
Result:

Inhibited PAR2-mediated ERK1/2 activation in HEK293 cells.

In Vivo

I-287 (50 mg/kg for p.o.) reduces Complete Freund's adjuvant (HY-153808)-induced inflammation in C57BL/6J mice^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

CFA-induced paw inflammation in adult male C57BL/6J mice ^[1]
Dosage:

50 mg/kg
Administration:

Oral gavage (p.o.) following the CFA
Result:

Reduces CFA-induced inflammation in C57BL/6J mice

Chemical Information

CAS No. 2014368-93-3
Appearance Solid
Masse moléculaire 565.04
Formule C₃₀H₃₀ClFN₄O₄
Color White to off-white
SMILES

O=C(C1=CN=C(N2CCN(C(C)(C2)C)C(C3=CC(N=C(C4=CC=C(C(F)=C4)Cl)C=C5C(C)(C)C)=C5O3)=O)C=C1)O
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvant et solubilité

In Vitro:

DMSO : 100 mg/mL (176.98 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.7698 mL

8.8489 mL

17.6979 mL

5 mM

0.3540 mL

1.7698 mL

3.5396 mL

10 mM

0.1770 mL

0.8849 mL

1.7698 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (4.42 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (4.42 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (4.42 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (275 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Avet C, et.al. The PAR2 inhibitor I-287 selectively targets Gαq and Gα12/13 signaling and has anti-inflammatory effects. Commun Biol. 2020 Nov 27;3(1):719. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.7698 mL	8.8489 mL	17.6979 mL	44.2447 mL
	5 mM	0.3540 mL	1.7698 mL	3.5396 mL	8.8489 mL
	10 mM	0.1770 mL	0.8849 mL	1.7698 mL	4.4245 mL
	15 mM	0.1180 mL	0.5899 mL	1.1799 mL	2.9496 mL
	20 mM	0.0885 mL	0.4424 mL	0.8849 mL	2.2122 mL
	25 mM	0.0708 mL	0.3540 mL	0.7079 mL	1.7698 mL
	30 mM	0.0590 mL	0.2950 mL	0.5899 mL	1.4748 mL
	40 mM	0.0442 mL	0.2212 mL	0.4424 mL	1.1061 mL
	50 mM	0.0354 mL	0.1770 mL	0.3540 mL	0.8849 mL
	60 mM	0.0295 mL	0.1475 mL	0.2950 mL	0.7374 mL
	80 mM	0.0221 mL	0.1106 mL	0.2212 mL	0.5531 mL
	100 mM	0.0177 mL	0.0885 mL	0.1770 mL	0.4424 mL

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I-287

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Voir tous les produits spécifiques à Isoform Protease Activated Receptor (PAR)

Voir tous les produits spécifiques à Isoform ERK

Activité biologique

Chemical Information

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

I-287 Related Classifications

HY-148016 Related Classifications