GD134 (GD-134)

Chemical Structure : GD134

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货号: PC-28130Not For Human Use, Lab Use Only.

GD134 (GD-134) is a potent, selective dual histamine H1 and H4 receptors (H1R/H4R) ligand / antagonist with pKi of 7.54 and 7.67 (hH1R/hH4R), shows 5-fold selectivity over hH3R and high selectivity over hH2R.

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生物&药学活性

GD134 (GD-134) is a potent, selective dual histamine H1 and H4 receptors (H1R/H4R) ligand / antagonist with pKi of 7.54 and 7.67 (hH1R/hH4R), shows 5-fold selectivity over hH3R and high selectivity over hH2R.
GD134 shows antagonistic activity on H1R and H4R with pEC50 values 6.03 and 5.84 at human H1R and mouse H1R, respectively in cAMP response element (CRE)-luciferase reporter gene assays.
GD134 demonstrates robust in vivo efficacy in a ragweed-induced mouse model of allergic conjunctivitis, significantly reducing hyperemia and outperforming selective H1R or H4R antagonists.

物理化学性质&存储条件

分子量	415.93
分子式	C18H24ClF2N5S
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	6,6-Difluoro-2-(4-methylpiperazin-1-yl)- N -(thiophen-2-ylmethyl)-5,6,7,8-tetrahydroquinazolin-4-amine hydrochloride

参考文献

1. Weber P, et al. J Med Chem. 2026 Sep 10;69(17):20967-21003.

GD134 (GD-134)

生物&药学活性

物理化学性质&存储条件

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GD134 (GD-134)

生物&药学活性

物理化学性质&存储条件

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