Ciproxifan maleate

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Ciproxifanmaleate(FUB-359maleate) 是一种高效、选择性组胺 H3 受体拮抗剂，IC50 为 9.2 nM，对其他受体亚型具有低表观亲和力。

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.

Ciproxifan inhibits [3H]HA release from synaptosomes of rat cerebral cortex, with a Ki of 0.5 nM.Ciproxifan (0.01 nM-1 μM; 60 min) inhibits the binding of [125I]iodoproxyfan with rat striatal membranes, with a Ki of 0.7 nM.

Ciproxifan (1 mg/kg; a single p.o.) increases the t-MeHA level in mouse brain, with an ED50 of 0.14 mg/kg.Ciproxifan (3 mg/kg, i.p.) improves the accuracy of responding in the five-choice task in rats only when the stimulus duration is 0.25 sec instead of 0.50 sec.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 (1 mg/kg; a single i.v.) decreases the H3-receptor ligand concentration in serum in mice, with the half-lives (t1/2) of 13 and 87 min for the distribution and elimination phases in mice, respectively.Ciproxifan (1 mg/kg; a single p.o.) exhibits oral bioavailability (F=62%) and maximal concentration (Cmax=420 nM) in mice.

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GPCR/G Protein

Histamine Receptor

H3 receptor

Neurological Disease

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184025-19-2

386.4

C20H22N2O6

>98% (HPLC)

DMSO: 10 mM

C1CC1C(=O)C2=CC=C(C=C2)OCCCC3=CN=CN3.C(=C\C(=O)O)\C(=O)O

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(-20℃)

With Ice Pack

≥ 2 years