Ciproxifan maleate
Based on 1 Customer Validation
Ciproxifan maleate (FUB 359 maleate) is a potent, selective, orally bioavailable and competitive antagonist of histamine H3-receptor, with an IC50 of 9.2 nM. Ciproxifan maleate displays low apparent affinity at other receptor subtypes. Ciproxifan maleate can be used for the research of aging disorders and Alzheimer's disease.
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- Pureté : 99.68%
- CAS No.: 184025-19-2
- Formule: C20H22N2O6
- Masse moléculaire:386.40
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Stockage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
IC50 & Target
[1]|
H3 receptor 9.2 nM (IC50) |
In Vitro
Ciproxifan inhibits [3H]HA release from synaptosomes of rat cerebral cortex, with a Ki of 0.5 nM[1].
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[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
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[1].
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 (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[1].
Ciproxifan (1 mg/kg; a single p.o.) exhibits oral bioavailability (F=62%) and maximal concentration (Cmax=420 nM) in mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 184025-19-2
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Appearance Solid
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Masse moléculaire 386.40
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Formule C20H22N2O6
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Color White to off-white
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SMILES
O=C(C1CC1)C2=CC=C(OCCCC3=CNC=N3)C=C2.O=C(O)/C=C\C(O)=O
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Synonyms
FUB 359 maleate
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvant et solubilité
In Vitro:
DMSO : ≥ 100 mg/mL (258.80 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 3.57 mg/mL (9.24 mM; ultrasonic and warming and heat to 60°C)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.47 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.47 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocole
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Alzheimer’s Disease Modeling
Alzheimer’s Disease (AD) is a neurodegenerative disorder characterized by a progressive decline in cognitive functions and loss of specific types of neurons and synapses. Alzheimer's symptoms can be simulated in mice by injecting drugs (such as Aβ) or genetically modified.
Pureté et documentation
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Fiche technique (277 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Ligneau X, et, al. Neurochemical and behavioral effects of ciproxifan, a potent histamine H3-receptor antagonist. J Pharmacol Exp Ther. 1998 Nov;287(2):658-66. [Content Brief]
[2]. Motawaj M, Arrang JM. Ciproxifan, a histamine H3-receptorantagonist / inverse agonist, modulates methamphetamine-induced sensitization in mice. Eur J Neurosci. 2011 Apr;33(7):1197-204. doi: 10.1111/j.1460-9568.2011.07618.x. [Content Brief]
[3]. Bardgett ME, Davis NN, Schultheis PJ, Griffith MS. Ciproxifan, an H3 receptor antagonist, alleviates hyperactivity and cognitive deficits in the APP Tg2576 mouse model of Alzheimer's disease. Neurobiol Learn Mem. 2011 Jan;95(1):64-72. [Content Brief]
[4]. Bardgett ME, Points M, Kleier J, Blankenship M, Griffith MS. The H3 antagonist, ciproxifan, alleviates the memory impairment but enhances the motor effects of MK-801 (dizocilpine) in rats. Neuropharmacology. 2010 Nov;59(6):492-502. [Content Brief]
[5]. Day M, et al . Differential effects of ciproxifan and nicotine on impulsivity and attention measures in the 5-choice serial reaction time test. Biochem Pharmacol. 2007 Apr 15;73(8):1123-34. [Content Brief]
[6]. Pillot C, Héron A, Schwartz JC, Arrang JM. Ciproxifan, a histamine H3-receptor antagonist/inverse agonist, modulates the effects of methamphetamine on neuropeptide mRNA expression in rat striatum. Eur J Neurosci. 2003 Jan;17(2):307-14. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| H2O / DMSO | 1 mM | 2.5880 mL | 12.9400 mL | 25.8799 mL | 64.6998 mL |
| 5 mM | 0.5176 mL | 2.5880 mL | 5.1760 mL | 12.9400 mL | |
| DMSO | 10 mM | 0.2588 mL | 1.2940 mL | 2.5880 mL | 6.4700 mL |
| 15 mM | 0.1725 mL | 0.8627 mL | 1.7253 mL | 4.3133 mL | |
| 20 mM | 0.1294 mL | 0.6470 mL | 1.2940 mL | 3.2350 mL | |
| 25 mM | 0.1035 mL | 0.5176 mL | 1.0352 mL | 2.5880 mL | |
| 30 mM | 0.0863 mL | 0.4313 mL | 0.8627 mL | 2.1567 mL | |
| 40 mM | 0.0647 mL | 0.3235 mL | 0.6470 mL | 1.6175 mL | |
| 50 mM | 0.0518 mL | 0.2588 mL | 0.5176 mL | 1.2940 mL | |
| 60 mM | 0.0431 mL | 0.2157 mL | 0.4313 mL | 1.0783 mL | |
| 80 mM | 0.0323 mL | 0.1617 mL | 0.3235 mL | 0.8087 mL | |
| 100 mM | 0.0259 mL | 0.1294 mL | 0.2588 mL | 0.6470 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Ciproxifan maleate Related Classifications
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