INCB38579
Based on 1 Customer Validation
INCB38579 is an orally active, highly brain penetrable, and selective histamine H4 receptor (HH4R) antagonist (hH4R IC50=4.8 nM, mH4R IC50=42 nM, rH4R IC50=32 nM). INCB38579 shows anti-inflammatory pain and anti-pruritic activities.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.33%
- No. CAS: 1246207-65-7
- Fòrmula: C25H34N6O
- Peso molecular:434.58
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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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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Ver todos los productos específicos de isoformas Histamine Receptor
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Actividad biológica
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Human H4 Receptor 4.8 nM (IC50) |
Mouse H4 Receptor 42 nM (IC50) |
Rat H4 receptor 21 nM (IC50) |
INCB38579 (0.1 nM-10 μM; 1.5 h) inhibits histamine binding to the recombinant human and rodent histamine H4 receptors[1].
INCB38579 (0.1 nM-10 μM; 20 min) blocks histamine-induced migration of dendritic cells differentiated from human monocytes and mouse bone marrow cells[1].
NCB38579 (0-30 nM; 1.5 h) inhibits histamine-induced cell shape change and migration of purified human eosinophils dose-dependently[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HEK293 cells
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Concentration:0.1 nM-10 μM
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Incubation Time:1.5 hours
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Result:Showed the IC50 values of 4.8, 42 and 21 nM for the human, mouse and rat histamine H4 receptors, respectively.
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Cell Line:Human monocytes, mouse bone marrow cells, and human eosinophils
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Concentration:0.1 nM-10 μM
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Incubation Time:20 min
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Result:Showed IC50s of 13.2 and 77 nM for human monocytes and mouse bone marrow cells，respectively.
Showed IC50 values of approximately 20-30 nM for purified human eosinophils.
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Cell Line:HEK293 cells
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Concentration:0-30 nM
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Incubation Time:1.5 hours
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Result:Showed the IC50 values of 4.8, 42 and 21 nM for the human, mouse and rat histamine H4 receptors, respectively.
INCB38579 (oral gavage; 100 mg/kg; once) shows antinociceptive functions in this acute model of inflammatory pain[1].
INCB38579 (oral gavage; 3, 10, 30, and 100 mg/kg; once) inhibits formalin-induced pain in rats and mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female CD-1 mice histamine-induced pruritus[1]
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Dosage:100 mg/kg
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Administration:Oral gavage; 100 mg/kg; once
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Result:Reduced the number of scratching bouts significantly (P<0.05).
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Animal Model:Sprague-Dawley rats injected with carrageenan[1]
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Dosage:100 mg/kg
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Administration:Oral gavage; 100 mg/kg; once
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Result:Increased the paw withdrawal threshold from a baseline of 61 g to approximately 100 g, achieving approximately 60% in maximal possible effect.
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Animal Model:Male Sprague–Dawley rats and male ICR mice injected with formalin into the hind paws[1]
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Dosage:3, 10, 30, and 100 mg/kg
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Administration:Oral gavage; 3, 10, 30, and 100 mg/kg; once
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Result:Showed a significant dose-dependent analgesic effect from 10 to 100 mg/kg in the phase 1 response and 30 to 100 mg/kg in the phase 2 response in the mouse formalin test.
Observed a dose-dependent and statistically significant effect in the phase 1 response, ranging from10 to 100 mg/kg, in the rat formalin test.
Chemical Information
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No. CAS 1246207-65-7
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Appearance Solid
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Peso molecular 434.58
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Fòrmula C25H34N6O
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Color Off-white to light yellow
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SMILES
O=C(CC1CCCC1)N2CCC3=CC=C(C4=NC(N)=NC(N5CCN(C)CC5)=C4)C=C3C2
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 230 mg/mL (529.25 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureza y Documentación
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Ficha de datos (277 KB)
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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)
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Instrucciones de manejo (2659 KB)
Referencias
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. 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 | 2.3011 mL | 11.5054 mL | 23.0107 mL | 57.5268 mL |
| 5 mM | 0.4602 mL | 2.3011 mL | 4.6021 mL | 11.5054 mL | |
| 10 mM | 0.2301 mL | 1.1505 mL | 2.3011 mL | 5.7527 mL | |
| 15 mM | 0.1534 mL | 0.7670 mL | 1.5340 mL | 3.8351 mL | |
| 20 mM | 0.1151 mL | 0.5753 mL | 1.1505 mL | 2.8763 mL | |
| 25 mM | 0.0920 mL | 0.4602 mL | 0.9204 mL | 2.3011 mL | |
| 30 mM | 0.0767 mL | 0.3835 mL | 0.7670 mL | 1.9176 mL | |
| 40 mM | 0.0575 mL | 0.2876 mL | 0.5753 mL | 1.4382 mL | |
| 50 mM | 0.0460 mL | 0.2301 mL | 0.4602 mL | 1.1505 mL | |
| 60 mM | 0.0384 mL | 0.1918 mL | 0.3835 mL | 0.9588 mL | |
| 80 mM | 0.0288 mL | 0.1438 mL | 0.2876 mL | 0.7191 mL | |
| 100 mM | 0.0230 mL | 0.1151 mL | 0.2301 mL | 0.5753 mL |
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