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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。
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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。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 183 | 现货 | |
5 mg | ¥ 395 | 现货 | |
10 mg | ¥ 567 | 现货 | |
25 mg | ¥ 1,150 | 现货 | |
50 mg | ¥ 1,860 | 现货 | |
100 mg | ¥ 2,780 | 现货 | |
200 mg | ¥ 3,970 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 393 | 现货 |
产品描述 | BRL 54443 is a potent 5-HT1E/1F receptor agonist (pKi values are 8.7 and 8.9 respectively). |
靶点活性 | 5-HT1D:7.2(pKi), 5-HT1A:7.2(pKi), 5-HT1B:6.9(pKi), 5-HT1F:9.25(pKi), 5-HT1E:8.7(pKi) |
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。 |
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. |
别名 | BRL54443 |
分子量 | 230.31 |
分子式 | C14H18N2O |
CAS No. | 57477-39-1 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||||||||||||
溶解度信息 | H2O: < 1 mg/mL (insoluble or slightly soluble) Ethanol: 2 mg/mL (8.68 mM) DMSO: 43 mg/mL (186.7 mM) | ||||||||||||||||||||||||||||||||||||||||
溶液配制表 | |||||||||||||||||||||||||||||||||||||||||
Ethanol/DMSO
DMSO
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