化合物BRL54443 T2459

Product Introduction
Bioactivity


英文名: BRL 54443

描述: BRL 54443 是一种有效的 5-HT1E/1F 受体激动剂，pKi 值分别为 8.7 和 8.9。

激酶实验: In Vitro Radiometric PKD Kinase Assay: The radiometric kinase assay is carried out by coincubating 0.5 μCi of [γ-32P]ATP, 20 μM ATP, 50 ng of purified recombinant human PKD (PKD1, PKD2, and PKD3) or CAMKIIα proteins, and 2.5 μg of Syntide-2 in 50 μl of kinase buffer that contains 50 mM Tris-HCl, pH 7.5, 4 mM MgCl2, 10 mM β-mercaptoethanol. The reaction is carried out under conditions that the initial rate is within the linear kinetic range. The filter papers are then washed three times in 0.5% phosphoric acid, air-dried, and counted using a Beckman LS6500 multipurpose scintillation counter.

体外活性: BRL54443相对于盐水,诱导最大胃内体积立即剂量依赖性增加.

体内活性: BRL 54443诱发收缩,其-logEC50为6.52。 BRL 54443引起的收缩很可能是通过刺激5-HT 5-HT 2A受体介导的。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: H2O : < 1 mg/mL (insoluble or slightly soluble)
Ethanol : 2 mg/mL (8.68 mM)
DMSO : 43 mg/mL (186.7 mM)


关键字: 5-HT Receptor | BRL 54443 | 5-hydroxytryptamine Receptor | Inhibitor | BRL-54443 | Serotonin Receptor | inhibit

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途