Chemical Structure : GD134
CAS No.:
GD134
(GD-134)
Catalog No.: 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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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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.
Physicochemical Properties
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M.Wt
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415.93
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Formula
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C18H24ClF2N5S
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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6,6-Difluoro-2-(4-methylpiperazin-1-yl)- N -(thiophen-2-ylmethyl)-5,6,7,8-tetrahydroquinazolin-4-amine hydrochloride
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References
1. Weber P, et al. J Med Chem. 2026 Sep 10;69(17):20967-21003.
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