Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ciproxifan maleate (FUB 359) 是一种选择性的,可口服和竞争性的组胺H3受体拮抗剂,IC50值为 9.2 nM。它对其他受体亚型的表观亲和力低,可用于研究衰老性疾病和阿尔兹海默症。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 267 | 现货 | ||
2 mg | ¥ 375 | 现货 | ||
5 mg | ¥ 672 | 现货 | ||
10 mg | ¥ 997 | 现货 | ||
25 mg | ¥ 1,980 | 现货 | ||
50 mg | ¥ 3,690 | 现货 | ||
100 mg | ¥ 5,270 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 677 | 现货 |
产品描述 | Ciproxifan maleate (FUB 359)(FUB-359 maleate) is a highly potent and selective histamin H3-receptor antagonist with IC50 of 9.2 nM, with low apparent affinity at other receptor subtypes. |
靶点活性 | H3 receptor:9.2 nM |
体外活性 | Ciproxifan inhibits [3H]HA release from synaptosomes with Ki of 0.5 nM. Ciproxifan inhibits the binding of [125I]iodoproxyfan at the brain H3 receptor with Ki of 0.7 nM. Ciproxifan displays high affinity at H3 receptor but shows low apparent affinity at other receptor subtypes as evaluated in functional tests on isolated organs (histamine H1 and H2, muscarinic M3, adrenergic α1D and β1, serotonin 5-HT1B, 5-HT2A, 5-HT3 and 5-HT4). [1] |
体内活性 | Ciproxifan intravenously injected at dose of 1 mg/kg decreases the H3-receptor ligand concentration in serum in Male Swiss mice, with half-times of distribution phase of 13min and elimination phase of 87 min, respectively. Ciproxifan (1 mg/kg, p.o.) rises brain t-MeHA level rapidly in Male Swiss mice, being already significantly increased after 30 min, reaching a plateau between 90 and 180 min and still remaining enhanced after 270 min. Ciproxifan leads to ED50 values of 0.23 mg/kg in cerebral cortex, 0.28 mg/kg in striatum and 0.30 mg/kg in hypothalamus in Male Wistar rats. Ciproxifan (3 mg/kg, i.p.) significantly increases choice accuracy as evaluated in the five-choice task performed using a short stimulus duration. Ciproxifan (0.15-2 mg/kg, p.o.) induces marked signs of neocortical electroencephalogram activation manifested by enhanced fast-rhythms density and an almost total waking state in cats. [1] Ciproxifan (10 mg/kg i.p.) enhances prepulse inhibition in the DBA/2 strain mice. [3] Ciproxifan (3 mg/kg i.p.) alleviates hyperactivity and cognitive deficits in the APP Tg2576 mouse model of Alzheimer's disease. [4] Ciproxifan (3 mg/kg i.p.) improves accuracy and decreased impulsivity in adult male hooded Lister rats. [5] |
别名 | FUB 359 maleate, FUB 359 |
分子量 | 386.4 |
分子式 | C20H22N2O6 |
CAS No. | 184025-19-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: 54 mg/mL (139.75 mM)
DMSO: 10 mM
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
Ethanol / DMSO | 1 mM | 2.588 mL | 12.94 mL | 25.8799 mL | 64.6998 mL |
5 mM | 0.5176 mL | 2.588 mL | 5.176 mL | 12.94 mL | |
10 mM | 0.2588 mL | 1.294 mL | 2.588 mL | 6.47 mL | |
Ethanol | 20 mM | 0.1294 mL | 0.647 mL | 1.294 mL | 3.235 mL |
50 mM | 0.0518 mL | 0.2588 mL | 0.5176 mL | 1.294 mL | |
100 mM | 0.0259 mL | 0.1294 mL | 0.2588 mL | 0.647 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。
Ciproxifan maleate 184025-19-2 GPCR/G Protein Immunology/Inflammation Neuroscience Histamine Receptor Inhibitor FUB-359 Maleate aging FUB359 Maleate inhibit Ciproxifan disorders FUB 359 maleate FUB 359 FUB359 histamine FUB-359 Ciproxifan Maleate FUB 359 Maleate Alzheimer's inhibitor