| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| Other Sizes |
Purity: ≥98%
Ciproxifan (formerly known as FUB-359) is a highly potent and selective histamine H3-receptor antagonist with IC50 of 9.2 nM, with low apparent affinity at other receptor subtypes. In addition, Ciproxifan has been reported to competitively antagonize the (R) α-MeHA induced relaxation of electrically stimulated guinea pig ileum longitudinal muscle. Besides, Ciproxifan has been revealed to have the effect on [125I]iodoproxyfan binding with a Ki value of 0.7±0.2 nM.
| ln Vitro |
Using a Ki of 0.5 nM, ciprofan suppresses the release of [3H]HA from rat cerebral cortex synaptosomes[1]. [125I]iodoproxyfan's binding to rat striatal membranes is inhibited by ciprofan (0.01 nM-1 μM; 60 minutes) with a Ki of 0.7 nM [1].
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| ln Vivo |
In the mouse brain, ciprofloxan (1 mg/kg; single oral dose) raises t-MeHA levels with an ED50 of 0.14 mg/kg[1]. In rats, ciprofen (3 mg/kg, i.p.) increased response accuracy in a five-choice task only when the stimulus duration was 0.25 seconds rather than 0.50 seconds [1]. Cats given ciprofen (0.15-2 mg/kg; oral) exhibit definite evidence of neocortical EEG activation, as evidenced by an increase in the density of fast rhythms and near-complete wakefulness [1]. The half-lives (t1/2) of the distribution and elimination phases in mice are 13 and 87 minutes, respectively, and ciprofen (1 mg/kg; single intravenous injection) can lower the concentration of H3 receptor ligands in the serum [1]. Mice show oral bioavailability (F=62%) and maximum concentration (Cmax=420 nM) for ciprofen (1 mg/kg; single oral dose) [1].
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| Animal Protocol |
Animals: 12-14 month old APPTg2576 transgenic mice and wild-type littermates (both genders) were used. Genotyping was confirmed by PCR. [3]
Dosing and administration: Ciproxifan was dissolved in saline. Mice received intraperitoneal injections at a dose of 3.0 mg/kg body weight. In the locomotor and swim maze study (between-subjects design), mice received daily injections beginning one week prior to testing and 30 minutes prior to testing each day over three weeks. In the object recognition study (within-subjects, counterbalanced design), mice received injections 30 minutes prior to each test session. [3] Locomotor activity testing: Mice were placed in activity frames for 60 minutes with lights off, over 5 consecutive days. Testing was conducted between 8:00 a.m. and 2:00 p.m. [3] Swim maze: A circular stainless steel tank (114 cm diameter) with opaque water was used. Hidden platform training: platform submerged 2 cm below water surface. Mice received 4 trials/day for 5 days, with a 5-minute intertrial interval. Escape latency, path length, swim speed, and average distance from platform were recorded. Probe trials: conducted 1 hour and 48 hours after the last training trial, with platform removed; number of platform crossings and time spent in the former platform area were recorded. Visible platform training: platform marked with a foil-wrapped Styrofoam ball, location changed daily; 4 trials/day for 3 days. [3] Novel object recognition: Apparatus: 60 × 60 × 60 cm gray wooden box. Habituation: 3 days of 15-minute exposure to empty apparatus. Testing: 5-minute trial with two identical objects, followed by a 5-minute delay, then a 3-minute trial with one familiar and one novel object. Object investigation was defined as being within 2 cm and oriented within 45 degrees of the object or having one paw on it. [3] |
| References |
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| Molecular Formula |
C20H22N2O6
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|---|---|
| Molecular Weight |
386.404
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| Exact Mass |
386.147
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| Elemental Analysis |
C, 62.17; H, 5.74; N, 7.25; O, 24.84
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| CAS # |
184025-19-2
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| Related CAS # |
Ciproxifan;184025-18-1
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| PubChem CID |
16219152
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| Appearance |
White to off-white solid powder
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| Boiling Point |
743.6ºC at 760 mmHg
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| Flash Point |
403.5ºC
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| Vapour Pressure |
3.22E-23mmHg at 25°C
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| LogP |
2.725
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
28
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| Complexity |
441
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(C1C([H])=C([H])C(=C([H])C=1[H])OC([H])([H])C([H])([H])C([H])([H])C1=C([H])N=C([H])N1[H])C1([H])C([H])([H])C1([H])[H].O([H])C([H])=O.O([H])C(C([H])=C([H])[H])=O
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| InChi Key |
RLQFKEYRALXXEJ-BTJKTKAUSA-N
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| InChi Code |
InChI=1S/C16H18N2O2.C4H4O4/c19-16(12-3-4-12)13-5-7-15(8-6-13)20-9-1-2-14-10-17-11-18-145-3(6)1-2-4(7)8/h5-8,10-12H,1-4,9H2,(H,17,18)1-2H,(H,5,6)(H,7,8)/b2-1-
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| Chemical Name |
Cyclopropyl-(4-(3-1H-imidazol-4-yl)propyloxyphenyl)ketone maleate
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| Synonyms |
FUB-359 FUB 359 FUB359 Ciproxifan. Ciproxifan maleate
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ≥ 100 mg/mL (~258.80 mM)
H2O : ~3.57 mg/mL (~9.24 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.47 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.47 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.47 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5880 mL | 12.9400 mL | 25.8799 mL | |
| 5 mM | 0.5176 mL | 2.5880 mL | 5.1760 mL | |
| 10 mM | 0.2588 mL | 1.2940 mL | 2.5880 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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