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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.33%
- CAS 番号: 1246207-65-7
- 分子式: C25H34N6O
- 分子量:434.58
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保管条件: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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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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Histamine Receptor アイソフォーム固有の製品をすべて表示
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生物活性
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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.
化学情報
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CAS 番号 1246207-65-7
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性状 Solid
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分子量 434.58
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (277 KB)
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SDS (251 KB)
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取扱説明書 (2659 KB)
参考文献
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 |
INCB38579 関連分類
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