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Ciproxifan Maleate Histamine Receptor antagonist

Name: Ciproxifan Maleate
Brand: Selleck Chemicals
SKU: S2813
Rating: 5 (2 reviews)

Cat.No.S2813

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 Structure

Molecular Weight: 386.4

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Quality Control

Batch: S281301 DMSO]54 mg/mL]false]Ethanol]54 mg/mL]false]Water]1 mg/mL]false Purity: 100%

Cited in Nature Medicine for its top-tier quality
COA
NMR
HPLC
SDS
Datasheet

100

Related Targets	Adrenergic Receptor AChR 5-HT Receptor COX Calcium Channel Dopamine Receptor GABA Receptor TRP Channel Cholinesterase (ChE) GluR
Other Histamine Receptor Inhibitors	GSK2879552 Dihydrochloride JNJ-7777120 Ebastine Mianserin HCl Astemizole Lafutidine Mizolastine Rupatadine Fumarate Betahistine 2HCl Levodropropizine

Chemical Information, Storage & Stability

Molecular Weight	386.4	Formula	C₁₆H₁₈N₂O₂.C₄H₄O₄	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	184025-19-2	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	FUB 359			Smiles	C1CC1C(=O)C2=CC=C(C=C2)OCCCC3=CN=CN3.C(=CC(=O)O)C(=O)O

Solubility

In vitro
Batch:

DMSO : 54 mg/mL (139.75 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 54 mg/mL

Water : 1 mg/mL

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
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Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

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% DMSO + % + % Tween 80 + % ddH₂O

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	Histamine H3 receptor 9.2 nM
In vitro	Ciproxifan inhibits [³H]HA release from synaptosomes with K_i of 0.5 nM. Ciproxifan inhibits the binding of [¹²⁵I]iodoproxyfan at the brain H3 receptor with K_i 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 α_1D and β₁, serotonin 5-HT_1B, 5-HT_2A, 5-HT₃ and 5-HT₄).
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. 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.
References	[1] https://pubmed.ncbi.nlm.nih.gov/9808693/ [2] https://pubmed.ncbi.nlm.nih.gov/12177222/ [3] https://pubmed.ncbi.nlm.nih.gov/15219708/ [4] https://pubmed.ncbi.nlm.nih.gov/21073971/ [5] https://pubmed.ncbi.nlm.nih.gov/17214974/

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