AC-264613
Based on 1 Customer Validation
AC-264613 is a potent and selective protease-activated receptor (PAR-2) agonist with a pEC50 of 7.5.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 98.3%
- No. CAS: 1051487-82-1
- Fòrmula: C19H18BrN3O2
- Peso molecular:400.27
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Almacenamiento:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Actividad biológica
pEC50: 7.5 (PAR-2)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK-293T | EC50 |
30 nM
Compound: 12, AC-264613
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Agonist activity at human PAR2 expressed in HEK293T cells assessed as increase in intracellular calcium level by bioluminescence assay
Agonist activity at human PAR2 expressed in HEK293T cells assessed as increase in intracellular calcium level by bioluminescence assay
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[PMID: 23895492] |
| HEK-293T | EC50 |
30 nM
Compound: 12, AC-264613
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Agonist activity at human PAR2 expressed in HEK293T cells assessed as stimulation of cell proliferation after 5 days by beta-galactosidase assay
Agonist activity at human PAR2 expressed in HEK293T cells assessed as stimulation of cell proliferation after 5 days by beta-galactosidase assay
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[PMID: 23895492] |
| HEK-293T | EC50 |
30 nM
Compound: 12, AC-264613
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Agonist activity at human PAR2 expressed in HEK293T cells assessed as stimulation of phosphatidylinositol hydrolysis after 45 mins by scintillation counting analysis
Agonist activity at human PAR2 expressed in HEK293T cells assessed as stimulation of phosphatidylinositol hydrolysis after 45 mins by scintillation counting analysis
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[PMID: 23895492] |
AC-264613 (10 μM; for 6 hours) causes a decrease of IRF5 expression and also significantly reduces p53 protein expression in macrophages[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Granulocyte-macrophage colony-stimulating factor (GM-CSF)-dependent macrophages
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Concentration:10 μM
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Incubation Time:6 hours
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Result:Significantly decreased IRF5 expression and reduced p53 protein levels.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 1051487-82-1
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Appearance Solid
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Peso molecular 400.27
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Fòrmula C19H18BrN3O2
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Color White to off-white
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SMILES
O=C(N/N=C(C1=CC=CC(Br)=C1)\C)[C@H]2[C@@H](CNC2=O)C3=CC=CC=C3
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvente y solubilidad
DMSO : ≥ 40 mg/mL (99.93 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureza y Documentación
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Ficha de datos (275 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Jimmi Gerner Seitzberg, et al. Discovery of potent and selective small-molecule PAR-2 agonists. J Med Chem. 2008 Sep 25;51(18):5490-3. [Content Brief]
[2]. Rui Yamaguchi, et al. A protease-activated receptor 2 agonist (AC-264613) suppresses interferon regulatory factor 5 and decreases interleukin-12p40 production by lipopolysaccharide-stimulated macrophages: Role of p53. Cell Biol Int. 2016 Jun;40(6):629-41 [Content Brief]
[3]. Luis R Gardell, et al. Identification and characterization of novel small-molecule protease-activated receptor 2 agonists. J Pharmacol Exp Ther. 2008 Dec;327(3):799-808. [Content Brief]
Complete Stock Solution Preparation Table
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 (sealed storage, away from moisture). 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 | 2.4983 mL | 12.4916 mL | 24.9831 mL | 62.4578 mL |
| 5 mM | 0.4997 mL | 2.4983 mL | 4.9966 mL | 12.4916 mL | |
| 10 mM | 0.2498 mL | 1.2492 mL | 2.4983 mL | 6.2458 mL | |
| 15 mM | 0.1666 mL | 0.8328 mL | 1.6655 mL | 4.1639 mL | |
| 20 mM | 0.1249 mL | 0.6246 mL | 1.2492 mL | 3.1229 mL | |
| 25 mM | 0.0999 mL | 0.4997 mL | 0.9993 mL | 2.4983 mL | |
| 30 mM | 0.0833 mL | 0.4164 mL | 0.8328 mL | 2.0819 mL | |
| 40 mM | 0.0625 mL | 0.3123 mL | 0.6246 mL | 1.5614 mL | |
| 50 mM | 0.0500 mL | 0.2498 mL | 0.4997 mL | 1.2492 mL | |
| 60 mM | 0.0416 mL | 0.2082 mL | 0.4164 mL | 1.0410 mL | |
| 80 mM | 0.0312 mL | 0.1561 mL | 0.3123 mL | 0.7807 mL |
AC-264613 Related Classifications
HY-14351 Related Classifications
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