首页 GPCR/G Protein Histamine Receptor Ciproxifan maleate
Ciproxifan maleate
编号 T2004     别名: FUB 359 maleate, FUB 359
CAS 184025-19-2     分子式 C20H22N2O6     分子量 386.4
靶点: H3 receptor;
Ciproxifan maleate(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.
选择批次  
规格 库存 单价 数量
2 mg 上海现货 408.00
5 mg 上海现货 736.00
10 mg 上海现货 1107.00
50 mg 上海现货 4527.00
100 mg 上海现货 6337.00
1 mL * 10 mM (in DMSO) 上海现货 736.00
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生物活性

产品描述

Ciproxifan maleate(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,9.2nM

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]

动物实验

动物模型:Swiss mice

化学信息

分子量

386.4

分子式

C20H22N2O6

CAS

184025-19-2

溶解度

DMSO: 10 mM

Ethanol: 54 mg/mL (139.75 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

储存条件

store at -80°C

备注

For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

配制溶液

1 mg 5 mg 10 mg
1 mM 2.588 ml 12.94 ml 25.88 ml
5 mM 0.518 ml 2.588 ml 5.176 ml
10 mM 0.259 ml 1.294 ml 2.588 ml
50 mM 0.052 ml 0.259 ml 0.518 ml
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