INCB38579

目录号: PL14944 纯度: ≥99%
INCB38579 是一种具有口服活性、高度脑穿透和选择性的组胺 H4 受体 (HH4R) 拮抗剂 (hH4R IC50=4.8 nM, mH4R IC50=42 nM, rH4R IC50=32 nM)。INCB38579 具有抗炎和抗瘙痒的活性。
CAS No. :1246207-65-7
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中文名称
INCB38579
英文名称
INCB38579
英文别名
Ethanone, 1-[7-[2-amino-6-(4-methyl-1-piperazinyl)-4-pyrimidinyl]-3,4-dihydro-2(1H)-isoquinolinyl]-2-cyclopentyl-;INCB38579
Cas No.
1246207-65-7
分子式
C25H34N6O
分子量
434.58
包装储存
Powder -20°C 3 years;4°C 2 years
详情描述
INCB38579 是一种具有口服活性、高度脑穿透和选择性的组胺 H4 受体 (HH4R) 拮抗剂 (hH4R IC50=4.8 nM, mH4R IC50=42 nM, rH4R IC50=32 nM)。INCB38579 具有抗炎和抗瘙痒的活性。
产品详情
INCB38579 是一种具有口服活性、高度脑穿透和选择性的组胺 H4 受体 (HH4R) 拮抗剂 (hH4R IC50=4.8 nM, mH4R IC50=42 nM, rH4R IC50=32 nM)。INCB38579 具有抗炎和抗瘙痒的活性。
生物活性
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.
性状
Solid
IC50 & Target[1][2]
Human H4 Receptor 4.8 nM (IC50) Mouse H4 Receptor
体外研究(In Vitro)
INCB38579 (0.1 nM-10 μM; 1.5 h) inhibits histamine binding to the recombinant human and rodent histamine H4 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. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Niu Shin, et al. INCB38579, a novel and potent histamine H? receptor small molecule antagonist with anti-inflammatory pain and anti-pruritic functions. Eur J Pharmacol. 2012 Jan 30;675(1-3):47-56.
溶解度数据
In Vitro: DMSO : 230 mg/mL (529.25 mM; ultrasonic and warming and heat to 60°C)配制储备液
搜索质检报告(COA)
[1]. Niu Shin, et al. INCB38579, a novel and potent histamine H? receptor small molecule antagonist with anti-inflammatory pain and anti-pruritic functions. Eur J Pharmacol. 2012 Jan 30;675(1-3):47-56.

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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