I-287 |
| Katalog-Nr.GC73145 |
I-287 ist ein oral aktiver selektiver PAR2-Inhibitor, der als negativer allosterischer Regulator auf die Aktivität von Gαq und Gα12/13 und deren nachgeschalteten Effektoren wirkt.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2014368-93-3
Sample solution is provided at 25 µL, 10mM.
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I-287 is a orally active selective PAR2 inhibitor that acting as a negative allosteric regulator on Gαq and Gα12/13 activity and their downstream effectors. I-287 reduces Complete Freund's adjuvant -induced inflammation in mice and can be used for inflammation/immunology research.
I-287 (0-60 μM; 15-30 min) inhibits PAR2-mediated activation of Gαq and Gα12/13 but not Gi/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].
I-287 (50 mg/kg for p.o.) reduces Complete Freund's adjuvant -induced inflammation in C57BL/6J mice[1].
References:
[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.
| Cas No. | 2014368-93-3 | SDF | |
| Formula | C30H30ClFN4O4 | M.Wt | 565.04 |
| Löslichkeit | DMSO : 100 mg/mL (176.98 mM; Need ultrasonic) | Storage | -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.7698 mL | 8.8489 mL | 17.6979 mL |
| 5 mM | 0.354 mL | 1.7698 mL | 3.5396 mL |
| 10 mM | 0.177 mL | 0.8849 mL | 1.7698 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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