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PF-03654764对人类H3受体具有高亲和力,并对大鼠H3受体具有较低亲和力,同时对其他人类组胺受体亚型(H1,H2和H4)具有超过1000倍的选择性。在使用报告基因测定法(β-内酰胺酶)并在稳定表达全长人类或大鼠H3受体的HEK293细胞中测量cAMP的功能性实验中,PF-03654764展示了强大的拮抗剂特性。
PF-03654764对人类H3受体具有高亲和力,并对大鼠H3受体具有较低亲和力,同时对其他人类组胺受体亚型(H1,H2和H4)具有超过1000倍的选择性。在使用报告基因测定法(β-内酰胺酶)并在稳定表达全长人类或大鼠H3受体的HEK293细胞中测量cAMP的功能性实验中,PF-03654764展示了强大的拮抗剂特性。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
10 mg | 询价 | 期货 | |
50 mg | 询价 | 期货 |
产品描述 | PF-03654764 exhibits high affinity for the human H3 receptor, but displays significantly lower affinity for the rat H3 receptor, with over 1000-fold selectivity against other human histamine receptor subtypes (H1, H2, and H4). In functional assays measuring cAMP using reporter gene assays (β-lactamase) conducted in HEK293 cells stably expressing the full-length human or rat H3 receptor, PF-03654764 demonstrated potent antagonist properties. |
别名 | Q27285769, OP970177FN |
分子量 | 350.46(free base) |
分子式 | C20H28F2N2O xC7H8O3S |
CAS No. | 1337536-85-2 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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