A-987306

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。

A-987306

CAS No. : 1082954-71-9

MCE 国际站：A-987306

产品活性：A-987306 是一种高效、有口服活性的组胺 H₄ 拮抗剂，对大鼠和人 H₄ 作用的 K_i 值分别为 3.4 nM 和 5.8 nM。 A-987306 在小鼠腹膜炎模型中显示出抗炎活性。

研究领域：GPCR/G Protein  |  Neuronal Signaling  |  Immunology/Inflammation

作用靶点：Histamine Receptor

In Vitro: A-987306 has potent functional antagonism in vitro at human, rat, and mouse H₄ receptors in cell-based FLIPR assays.
A-987306 is 620-fold, >1600-fold, and 162-fold selective for the human H₄R over the human H₁, H₂ , and H₃ receptors in cell-based Ca²⁺-flux functional assay (FLIPR).
A-987306 shows lower selectivity for H₄R in the rat (only 4-fold selective for the rat H₄R over the rat H₃R) in FLIPR.

In Vivo: A-987306 (98.23 μg/kg-9.82 mg/kg; i.p.) is found to reduce scratching induced by the histamine H₄ agonist clobenpropit (HY-101198).
A-987306 (10 mg/kg; p.o.) has a moderate fractional oral bioavailability (F_po/iv=26%) with a half-life of 3.7 h and a C_max of 0.30 µM at a T_max of 1.5 h after dosing.

相关产品：Histamine  |  Clemastine fumarate  |  Terfenadine  |  Amitriptyline hydrochloride  |  Astemizole  |  Cimetidine  |  Loratadine  |  Osthole  |  Mecamylamine hydrochloride  |  Diphenhydramine hydrochloride  |  Desloratadine  |  Doxepin Hydrochloride  |  Perphenazine  |  Ritanserin  |  Promethazine hydrochloride  |  Famotidine  |  Fexofenadine hydrochloride  |  Mianserin hydrochloride  |  (S)-(+)-Dimethindene maleate  |  Cetirizine dihydrochloride  |  Chlorpheniramine maleate  |  Ketotifen fumarate  |  Mepyramine maleate  |  Ranitidine hydrochloride  |  Benztropine mesylate  |  JNJ-7777120  |  Meclizine dihydrochloride  |  Lodoxamide  |  Mirtazapine

热门产品线：重组蛋白  |  化合物库  |  天然产物  |  荧光染料  |  PROTAC  |  同位素标记物

Trending products：Recombinant Proteins  |  Bioactive Screening Libraries  |  Natural Products  |  Dye Reagents  |  PROTAC  |  Isotope-Labeled Compounds