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Ciproxifan

Ciproxifan 更多供应商
公司名称: 上海波以尔化工有限公司  
联系电话:
产品介绍: 中文名称:Ciproxifan
英文名称:FUB359
CAS:184025-18-1
纯度:98%min
公司名称: 上海佰世凯化学科技有限公司  
联系电话: 021-20908456
产品介绍: 英文名称:FUB 359
CAS:184025-18-1
备注:C14471
公司名称: 上海景颜化工科技有限公司  
联系电话: 13817811078
产品介绍: 英文名称:FUB359
CAS:184025-18-1
纯度:98%
公司名称: Hangzhou Sage Chemical Co., Ltd.  
联系电话: 0571-86818502
产品介绍: 英文名称:Methanone, cyclopropyl[4-[3-(1H-iMidazol-4-yl)propoxy]phenyl]-
CAS:184025-18-1
纯度:98% 包装信息:1g;5g;100g;Bulk
公司名称: 上海遐瑞医药科技有限公司  
联系电话: +86 21 61551611
产品介绍: 英文名称:fub 359;Ciproxifan; cyclopropyl(4-(3-(1h-imidazol-5-yl)propoxy)phenyl)methanone
CAS:184025-18-1
纯度:98% 包装信息:50kg;25kg;10kg;5kg;500g;500mg; 备注:工业级/医药级
Ciproxifan
生物活性体外研究体内研究靶点
中文名称:Ciproxifan
中文同义词:环丙基[4-[3-(1H-咪唑-5-基)丙氧基]苯;环丙基[4-[3-(1H-咪唑-5-基)丙氧基]苯基]甲酮
英文名称:Ciproxifan
英文同义词:CS-757;Ciproxifan (FUB-359);Cyclopropyl[4-[3-(1H-imidazol-5-yl)propoxy]phenyl]methanone;FUB 359;Methanone, cyclopropyl[4-[3-(1H-iMidazol-4-yl)propoxy]phenyl]-;Ciproxifan, >=99%;Methanone, cyclopropyl[4-[3-(1H-imidazol-5-yl)propoxy]phenyl]-;Ciproxifan USP/EP/BP
CAS号:184025-18-1
分子式:C16H18N2O2
分子量:270.33
EINECS号:
相关类别:神经信号;小分子抑制剂,天然产物;Inhibitors
Mol文件:184025-18-1.mol
Ciproxifan
Ciproxifan 性质
沸点 526.9±35.0 °C(Predicted)
密度 1.231
溶解度 H2O: insoluble
形态solid
酸度系数(pKa)14.54±0.10(Predicted)
颜色white
Ciproxifan 用途与合成方法
生物活性Ciproxifan是一种高效的,选择性的histamin H3-receptor拮抗剂,IC50为9.2 nM,作用于其他受体亚型具有低亲和力。
体外研究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).
体内研究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. Ciproxifan (10 mg/kg i.p.) enhances prepulse inhibition in the DBA/2 strain mice. Ciproxifan (3 mg/kg i.p.) alleviates hyperactivity and cognitive deficits in the APP Tg2576 mouse model of Alzheimer's disease. Ciproxifan (3 mg/kg i.p.) improves accuracy and decreased impulsivity in adult male hooded Lister rats.
靶点

H 3 receptor

9.2 nM (IC 50 )

安全信息
危险品标志 Xn
危险类别码 22-36/37/38-43
安全说明 26-36/37/39
WGK Germany 3
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