Ciproxifan maleate

SKU: orb1306772

Description

Ciproxifan maleate

Research Area

Immunology & Inflammation, Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 184025-19-2
• MW: 386.4
• Purity: 99.45%
• Formula: C₂₀H₂₂N₂O₆
• SMILES: OC(=O)\C=C/C(O)=O.O=C(C1CC1)c1ccc(OCCCc2c[nH]cn2)cc1
• Target: Histamine Receptor
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.18 mM);Ethanol:54 mg/mL (139.75 mM);DMSO:50 mg/mL (129.4 mM)

Bioactivity

• Target IC50:
  H3 receptor:9.2 nM
• In Vivo:
  Ciproxifan intravenously injected at dose of 1 mg/kg decrease the H3-receptor li and 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.
• In Vitro:
  Ciproxifan inhibits [3H]HA release from synaptosomes with Ki of 0.5 nM. Ciproxifan inhibit the binding of [125I]iodoproxyfan a 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).

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Disclaimer: For research use only

Alternative Names

Histamine Receptor, HistamineReceptor, FUB359, FUB-359, FUB359 Maleate, FUB-359 Maleate, FUB 359 maleate, H3 receptor, Ciproxifan, Alzheimer's, aging

Compound Identifiers

PubChem CID

16219152