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Ciproxifan Maleate

Ciproxifan Maleate

Item no.	S2813-5
Manufacturer	Selleckchem
CASRN	184025-19-2
Amount	5 mg
Quantity options	1 g 10 g 10 mM/1 ml 25 mg 5 mg 5 g
Category	Oncology Food Safety Histamines Neuroscience Metabolism Regulation of Appetite Aging & Neurological Disorders Protein Aggregation, Clearance & Misfolding Inhibitors & Compound Libraries Small Molecules By Organ Brain Cancer
Type	Inhibitors
Specific against	other
Smiles	C1CC1C(=O)C2=CC=C(C=C2)OCCCC3=CN=CN3.C(=CC(=O)O)C(=O)O
ECLASS 10.1	32160490
ECLASS 11.0	32160490
UNSPSC	12000000
Alias	FUB 359
Similar products	Ciproxifan
Available
Storage Conditions	2 years -80 in solvent
Molecular Weight	386, 4
Administration	Intravenous or oral adminstration
Animal Models	Male Swiss mice
Dosages	1 mg/kg
Formulation	1% methylcellulose for the oral route, in 0.9% NaCl for i.v. routes
IC50	9.2 nM [1], 9.2 nM [1], 9.2 nM [1], 9.2 nM [1], 9.2 nM [1], 9.2 nM [1]
In vitro	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 alpha1D and beta1, serotonin 5-HT1B, 5-HT2A, 5-HT3 and 5-HT4). [1]
In vivo	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 (0.15â€“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 mgg 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]
Kinase Assay	Histamine H3 receptor assay, Longitudinal muscle strips from guinea pig small intestine are dissected out and incubated in a gassed O2/CO2 (95%/5%) modified Krebs-Ringer's bicarbonate medium at 37 C in presence of 1 uM mepyramine to block the H1 receptor. After equilibration, contractile activity under stimulation (rectangular pulses of 15 V, 0.5 msec, 0.1 Hz) is recorded. Concentration-response curves of the effect of (R)alpha-MeHA alone or together with Ciproxifan are established.
Solubility (25C)	DMSO 54 mg/mL, Water 1 mg/mL, Ethanol 54 mg/mL
Information	Ciproxifan (FUB 359) is a highly potent and selective histamin H3-receptor antagonist with IC50 of 9.2 nM, with low apparent affinity at other receptor subtypes.
Chemical Name	Methanone, cyclopropyl[4-[3-(1H-imidazol-4-yl)propoxy]phenyl]-, (Z)-2-butenedioate (1:1)

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