Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Irdabisant (CEP-26401) 是选择性、口服活性和血脑屏障渗透性的组胺 H3 受体 (histamine H3 receptor, H3R) 拮抗剂/逆激动剂。Irdabisant 显示人 H3R 和大鼠 H3R 的 Ki 分别为 2.0 nM 和 7.2 nM。Irdabisant 抑制 hERG 电流的活性相对较低 (IC50= 13.8 μM)。在大鼠社会认知模型中,Irdabisant 具有认知增强和唤醒作用。Irdabisant 可用于研究精神分裂症或认知障碍。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 913 | 现货 | ||
5 mg | ¥ 2,320 | 现货 | ||
10 mg | ¥ 3,490 | 现货 | ||
25 mg | ¥ 5,730 | 现货 | ||
50 mg | ¥ 7,990 | 现货 | ||
100 mg | ¥ 10,700 | 现货 | ||
500 mg | ¥ 21,500 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,580 | 现货 |
产品描述 | Irdabisant (CEP-26401) (CEP-26401) is a selective, orally active and blood-brain barrier (BBB) penetrant antagonist/inverse agonist of histamine H3 receptor (H3R) (rat H3R Ki= 7.2 nM, human H3R Ki= 2.0 nM). Irdabisant exhibits relatively low inhibitory activity against hERG current (IC50= 13.8 μM). Irdabisant exhibits cognition-enhancing and wake-promoting activities in the rat social recognition model. Irdabisant can be used for research on schizophrenia or cognitive impairment. |
靶点活性 | H3 receptor (human):2 nM (Ki), H3 receptor (rat):7.2 nM (Ki) |
体外活性 | Irdabisant exhibits inverse agonist activity with EC50 values of 2.0 nM and 1.1 nM for rat H3R and human H3R, respectively; exhibits antagonist activity with Kb, app values of 1.0 nM and 0.4 nM for rat H3R and human H3R, respectively. Irdabisant exhibits moderate activity at Muscarinic M2 (Ki = 3.7 ± 0.0 μM) and Adrenergic α1A (Ki = 9.8 ± 0.3 μM) receptors, Norepinephrine transporters (Ki = 10 ± 1 μM), Dopamine transporters (Ki = 11 ± 2 μM), and phosphodiesterase PDE3 (IC50 = 15 ± 1 μM). Irdabisant inhibits the cytochrome P450 enzymes CYP1A2, 2C9, 2C19, 2D6, and 3A4 with IC50 values of greater than 30 μM, indicating less potential for drug-drug interactions[1]. |
体内活性 | Irdabisant (0.0001-0.1 mg/kg; i.v. or p.o.; single dosage) improves performance in the rat social recognition model of short-term memory. Irdabisant (0.01-0.3 mg/kg; p.o.; single dosage) dose-dependently inhibits H3R agonist RAMH-induced dipsogenia. Irdabisant (1 mg/kg for i.v. and 3 mg/kg for p.o.; single dosage) is rapidly absorbed with high oral bioavailability in rat and monkey, and exhibits a moderate clearance in monkey and dog compared to the rat[1]. Irdabisant (3-30 mg/kg; p.o.; single dosage) exhibits wake-promoting activity in rat. Irdabisant (3-30 mg/kg; i.p.) increases prepulse inhibition (PPI) in DBA/2NCrl mice[2]. |
别名 | CEP-26401, CEP 26401, CEP26401 |
分子量 | 313.39 |
分子式 | C18H23N3O2 |
CAS No. | 1005402-19-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 22.5 mg/mL (71.79 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 3.1909 mL | 15.9546 mL | 31.9091 mL | 79.7728 mL |
5 mM | 0.6382 mL | 3.1909 mL | 6.3818 mL | 15.9546 mL | |
10 mM | 0.3191 mL | 1.5955 mL | 3.1909 mL | 7.9773 mL | |
20 mM | 0.1595 mL | 0.7977 mL | 1.5955 mL | 3.9886 mL | |
50 mM | 0.0638 mL | 0.3191 mL | 0.6382 mL | 1.5955 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。
Irdabisant 1005402-19-6 GPCR/G Protein Immunology/Inflammation Neuroscience Histamine Receptor CEP-26401 CEP 26401 CEP26401 Inhibitor inhibitor inhibit