产品
编 号：F743491
分子式：C25H34N6O
分子量：434.58
分子式：C25H34N6O
分子量：434.58
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
1mg
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5mg
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10mg
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25mg
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结构图
CAS No: 1246207-65-7
产品详情
生物活性：
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.
体内研究：
INCB38579 (口服灌胃；100 mg/kg；一次) 抑制小鼠组胺介导的瘙痒症。INCB38579 (口服强饲法；100 mg/kg；一次) 在这种炎症性疼痛的急性模型中表现出镇痛功能。INCB38579 (口服灌胃；3、10、30 和 100 mg/kg；一次) 抑制大鼠和小鼠福尔马林诱导的疼痛。Animal Model:Female CD-1 mice histamine-induced pruritus
Dosage:100 mg/kg
Administration:Oral gavage; 100 mg/kg; once
Result:Reduced the number of scratching bouts significantly (P<0.05).
Animal Model:Sprague-Dawley rats injected with carrageenan
Dosage:100 mg/kg
Administration:Oral gavage; 100 mg/kg; once
Result:Increased the paw withdrawal threshold from a baseline of 61 g to approximately 100 g, achieving approximately 60% in maximal possible effect.
Animal Model:Male Sprague–Dawley rats and male ICR mice injected with formalin into the hind paws
Dosage:3, 10, 30, and 100 mg/kg
Administration:Oral gavage; 3, 10, 30, and 100 mg/kg; once
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.
体外研究：
INCB38579 (0.1 nM-10 μM；1.5 小时) 抑制组胺与重组人和啮齿动物组胺 H4 受体的结合。INCB38579 (0.1 nM-10 μM；20 分钟) 阻断组胺诱导的人单核细胞和小鼠骨髓细胞分化的树突状细胞迁移。NCB38579 (0-30 nM；1.5 小时) 剂量依赖性地抑制组胺诱导的细胞形状变化和纯化人嗜酸性粒细胞的迁移。
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.
体内研究：
INCB38579 (口服灌胃；100 mg/kg；一次) 抑制小鼠组胺介导的瘙痒症。INCB38579 (口服强饲法；100 mg/kg；一次) 在这种炎症性疼痛的急性模型中表现出镇痛功能。INCB38579 (口服灌胃；3、10、30 和 100 mg/kg；一次) 抑制大鼠和小鼠福尔马林诱导的疼痛。Animal Model:Female CD-1 mice histamine-induced pruritus
Dosage:100 mg/kg
Administration:Oral gavage; 100 mg/kg; once
Result:Reduced the number of scratching bouts significantly (P<0.05).
Animal Model:Sprague-Dawley rats injected with carrageenan
Dosage:100 mg/kg
Administration:Oral gavage; 100 mg/kg; once
Result:Increased the paw withdrawal threshold from a baseline of 61 g to approximately 100 g, achieving approximately 60% in maximal possible effect.
Animal Model:Male Sprague–Dawley rats and male ICR mice injected with formalin into the hind paws
Dosage:3, 10, 30, and 100 mg/kg
Administration:Oral gavage; 3, 10, 30, and 100 mg/kg; once
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.
体外研究：
INCB38579 (0.1 nM-10 μM；1.5 小时) 抑制组胺与重组人和啮齿动物组胺 H4 受体的结合。INCB38579 (0.1 nM-10 μM；20 分钟) 阻断组胺诱导的人单核细胞和小鼠骨髓细胞分化的树突状细胞迁移。NCB38579 (0-30 nM；1.5 小时) 剂量依赖性地抑制组胺诱导的细胞形状变化和纯化人嗜酸性粒细胞的迁移。
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