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首页-小分子抑制剂&激动剂-GPCR-Histamine Receptor-Izuforant
Izuforant

Chemical Structure : Izuforant

CAS No.: 1429374-83-3

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Izuforant (JW1601, LEO 152020)

货号: PC-23262Not For Human Use, Lab Use Only.

Izuforant (JW1601, LEO 152020) is a potent, selective and oral histamine 4 receptor (H4R) antagonist with IC50 of 65.1-72.2 nM in human whole-blood assay, and pKi of 6.83 and 5.36 at mouse and rat histamine receptor subtypes. shows lower pKi values against other histamine receptor.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

Izuforant (JW1601, LEO 152020) is a potent, selective and oral histamine 4 receptor (H4R) antagonist with IC50 of 65.1-72.2 nM in human whole-blood assay, and pKi of 6.83 and 5.36 at mouse and rat histamine receptor subtypes. shows lower pKi values against other histamine receptor.
Izuforant (JW1601, LEO 152020) inhibits eosinophil shape changes (ESC) induced by imetit, which mimics the histamine effect in triggering eosinophil changes
Izuforant (JW1601, LEO 152020) shows inhibitory effects in an antigen-specific Th2 type immune response, subsequently reducing Th2 cytokine-related skin inflammation and dermal thickness in the ear in a mouse model of epicutaneous sensitization and oxazolone-mediated AD.
Izuforant (JW1601, LEO 152020) has the potential to effectively control inflammation and pruritus.

物理化学性质&存储条件

分子量 334.18
分子式 C12H12BrN7
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

1-(8-bromopyrido[2,3-e][1,2,4]triazolo[4,3-a]pyrazin-4-yl)-N-methylazetidin-3-amine

参考文献

1. Grekowitz E, et al. Br J Dermatol. 2024 May 17;190(6):825-835.

2. Jin BH, et al. Clin Transl Sci. 2024 Oct;17(10):e70032.

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