INCB38579

COA

级别和纯度:

≥99%

CAS编号: 1246207-65-7
分子式: C₂₅H₃₄N₆O
分子量: 434.58

有货

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货号 (SKU)	包装规格	是否现货
I649402-5mg	5mg	期货
I649402-10mg	10mg	期货
I649402-25mg	25mg	期货
I649402-50mg	50mg	期货

查看相关系列

Class A GPCR (8201) GPCR/G Protein (3179) Histamine Receptor (192) Immunology/Inflammation (1938) 神经元信号传导 (3320)

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基本描述

规格或纯度	≥99%
英文名称	INCB38579
生化机理	INCB38579 是一种口服活性、高脑穿透性和选择性组胺 H 4 受体（HH 4 R）拮抗剂（hH 4 R IC 50 =4.8 nM，mH 4 R IC 50 =42 nM，rH 4 R IC 50 =32 nM）。INCB38579 具有抗炎痛和抗瘙痒活性。
储存温度	-20°C储存
运输条件	超低温冰袋运输
作用类型	拮抗剂
产品介绍	INCB38579 is an orally active, highly brain penetrable, and selective histamine H 4 receptor (HH 4 R) antagonist (hH 4 R IC 50 =4.8 nM, mH 4 R IC 50 =42 nM, rH 4 R IC 50 =32 nM). INCB38579 shows anti-inflammatory pain and anti-pruritic activities In Vitro INCB38579 (0.1 nM-10 μM; 1.5 h) inhibits histamine binding to the recombinant human and rodent histamine H 4 receptors. INCB38579 (0.1 nM-10 μM; 20 min) blocks histamine-induced migration of dendritic cells differentiated from human monocytes and mouse bone marrow cells. NCB38579 (0-30 nM; 1.5 h) inhibits histamine-induced cell shape change and migration of purified human eosinophils dose-dependently. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: HEK293 cells Concentration: 0.1 nM-10 μM Incubation Time: 1.5 hours Result: Showed the IC 50 values of 4.8, 42 and 21 nM for the human, mouse and rat histamine H 4 receptors, respectively. Cell Viability AssayCell Line: Human monocytes, mouse bone marrow cells, and human eosinophils Concentration: 0.1 nM-10 μM Incubation Time: 20 min Result: Showed IC 50 s of 13.2 and 77 nM for human monocytes and mouse bone marrow cells，respectively. Showed IC 50 values of approximately 20-30 nM for purified human eosinophils. Cell Viability AssayCell Line: HEK293 cells Concentration: 0-30 nM Incubation Time: 1.5 hours Result: Showed the IC 50 values of 4.8, 42 and 21 nM for the human, mouse and rat histamine H 4 receptors, respectively. In Vivo INCB38579 (oral gavage; 100 mg/kg; once) inhibits histamine-mediated pruritus in mice . INCB38579 (oral gavage; 100 mg/kg; once) shows antinociceptive functions in this acute model of inflammatory pain . INCB38579 (oral gavage; 3, 10, 30, and 100 mg/kg; once) inhibits formalin-induced pain in rats and mice . MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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. Form:Solid IC50& Target:Human H 4 Receptor 4.8 nM (IC 50 ) Mouse H 4 Receptor 42 nM (IC 50 ) Rat H 4 receptor 21 nM (IC 50 )
纯度	≥99%

化学和物理性质

溶解性	DMSO : 230 mg/mL (529.25 mM; ultrasonic and warming and heat to 60°C)

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INCB38579

库存信息

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基本描述

名称和识别符

化学和物理性质

质检证书（CoA,COO,BSE/TSE 和分析图谱)

溶液计算器

摩尔浓度计算器

稀释计算器

复溶计算器