Vergleich

Ciproxifan Maleate Europäischer Partner

ArtNr S2813-5
Hersteller Selleckchem
CAS-Nr. 184025-19-2
Menge 5 mg
Quantity options 1 g 10 g 10 mM/1 ml 25 mg 5 mg 5 g
Kategorie
Typ 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
Lieferbar
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 (0.15–2 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 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)

Hinweis: Die dargestellten Informationen und Dokumente (Bedienungsanleitung, Produktdatenblatt, Sicherheitsdatenblatt und Analysezertifikat) entsprechen unserem letzten Update und sollten lediglich der Orientierung dienen. Wir übernehmen keine Garantie für die Aktualität. Für spezifische Anforderungen bitten wir Sie, uns eine Anfrage zu stellen.

Alle Produkte sind nur für Forschungszwecke bestimmt. Nicht für den menschlichen, tierärztlichen oder therapeutischen Gebrauch.

Menge: 5 mg
Lieferbar: In stock
lieferbar

Vergleichen

Auf den Wunschzettel

Angebot anfordern

Lieferzeit anfragen

Technische Frage stellen

Bulk-Anfrage stellen

Fragen zum Produkt?