Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Idalopirdine Hydrochloride (Lu AE58054 Hydrochloride) 是一种选择性的5-HT6 受体拮抗剂,Ki 为 0.83 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 693 | 现货 | ||
2 mg | ¥ 973 | 现货 | ||
5 mg | ¥ 1,410 | 现货 | ||
10 mg | ¥ 2,130 | 现货 | ||
25 mg | ¥ 2,770 | 现货 | ||
50 mg | ¥ 4,130 | 现货 | ||
100 mg | ¥ 5,880 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,510 | 现货 |
产品描述 | Idalopirdine Hydrochloride (Lu AE58054 Hydrochloride) is an in-vivo binding affinity and effect, in-vitro selectivity and potency of 5-HT(6)R antagonist (Ki: 0.83 nM). |
靶点活性 | 5-HT6 receptor:0.83 nM(Ki) |
体外活性 | In the 5-HT(6) GTP gamma S efficacy assay, Lu AE58054 showed potent inhibition of 5-HT-mediated activation. Apart from medium affinity to adrenergic alpha (1B)- and alpha(1A)-adrenoreceptors, Lu AE58054 shows >50-fold selectivity compared with more than 70 targets examined[1]. |
体内活性 | In the rats model, Orally administered Lu AE58054 inhibited binding of the 5-HT6 antagonist Lu AE60157 (ED50: 2.7 mg/kg). Administration of Lu AE58054 in a dose range (5–20 mg/kg) leading to above 65% 5-HT6R binding, which reversed cognitive impairment in rats treatment with phencyclidine. These results indicate that Lu AE58054 is a potent antagonist of 5-HT6Rs with good oral bioavailability in the rat model of cognitive impairment in schizophrenia[1]. |
别名 | Lu AE58054盐酸盐, Lu AE58054 Hydrochloride, Idalopirdine HCl |
分子量 | 434.83 |
分子式 | C20H20ClF5N2O |
CAS No. | 467458-02-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: 50 mg/mL(114.99 mM)
DMSO: 20 mg/mL(45.99 mM)
H2O: 3 mg/mL(6.90 mM, with ultrasonic and warming), Sonification and heating are recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
Ethanol / DMSO / H2O | 1 mM | 2.2997 mL | 11.4987 mL | 22.9975 mL | 57.4937 mL |
5 mM | 0.4599 mL | 2.2997 mL | 4.5995 mL | 11.4987 mL | |
Ethanol / DMSO | 10 mM | 0.23 mL | 1.1499 mL | 2.2997 mL | 5.7494 mL |
20 mM | 0.115 mL | 0.5749 mL | 1.1499 mL | 2.8747 mL | |
Ethanol | 50 mM | 0.046 mL | 0.23 mL | 0.4599 mL | 1.1499 mL |
100 mM | 0.023 mL | 0.115 mL | 0.23 mL | 0.5749 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Idalopirdine Hydrochloride 467458-02-2 GPCR/G Protein Neuroscience 5-HT Receptor Serotonin Receptor Lu AE58054 inhibit 5-hydroxytryptamine Receptor Lu AE-58054 Hydrochloride Lu AE58054盐酸盐 Lu AE58054 Hydrochloride Lu AE-58054 Lu AE 58054 Hydrochloride Lu AE 58054 Idalopirdine HCl Idalopirdine Inhibitor inhibitor