| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg | |||
| 250mg | |||
| Other Sizes |
| Targets |
Fantofarone targets L-type calcium channels (voltage-gated calcium channels, Cav1.2), which are critical for calcium influx in cardiac and smooth muscle cells. As a non-competitive antagonist, fantofarone binds to a site distinct from the dihydropyridine binding site on the calcium channel. This mechanism provides potent inhibition of calcium currents and may offer advantages in terms of use-dependence and reduced side effects.
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| ln Vitro |
Compared to CQ, the intrinsic antimalarial characteristics of the calcium channel blockers VIZ and Fantofarone (SR) are evidently weaker, and they both seem to be marginally more effective against CQ-resistant parasites than against CQ-sensitive parasites. Strength. Interestingly, Fantofarone was approx. Ten times as powerful than elavil. When it comes to two strains of P. fdciparum, fantofarone (SR) is ten times more effective than the phenylalkylamine verapamil (VR). Both calcium channel blockers, with verapamil being two to three times more powerful than Fantofarone, increased the CQ-sensitive activity of CQ-resistant P. fufcipurum strains, as demonstrated by isobolograms. Additionally, when taken with identical IC50 subinhibitory fractions, VR reduces CQ resistance 2–3 times more effectively than Fantofarone [1].
In vitro, fantofarone potently inhibits L-type calcium channel currents in a non-competitive manner. The compound shows use-dependent blockade, with greater inhibition at higher stimulation frequencies. Fantofarone's effects on calcium currents have been characterized in isolated cardiac myocytes and smooth muscle cells using patch-clamp electrophysiology. The compound also exhibits anti-arrhythmic properties in various in vitro models. |
| ln Vivo |
Treatment with ventofalone (50 mg/kg, intravenous) or isosorbide dinitrate (0.3 mg/kg, intravenous) decreased the incidence and severity of vasospasm, while verapamil (0.2 mg/kg, intravenous injection) is far less effective. Isosorbide dinitrate largely prevented distal AIV, but it had no discernible effect on proximal diameter reduction. Fantofarone was found to be the most efficient drug in reducing both proximal and distal vasospasm. Throughout the experiment, this compound greatly decreased AIV. There is no discernible decrease in AIV with verapamil[2].
In vivo, fantofarone has demonstrated cardiovascular effects including vasodilation and negative inotropic effects. The compound's calcium channel blocking activity reduces peripheral vascular resistance and cardiac contractility. Fantofarone has been studied for its potential anti-arrhythmic and antihypertensive effects in animal models. The compound's non-competitive mechanism may offer advantages over competitive calcium channel blockers. |
| Enzyme Assay |
Non-cellular receptor binding assays for fantofarone involve competitive radioligand binding displacement studies using membrane preparations from tissues expressing L-type calcium channels. Membranes are incubated with a radiolabeled calcium channel ligand (e.g., [³H]nitrendipine or [³H]desmethoxyverapamil) and varying concentrations of fantofarone. Following incubation and filtration, bound radioactivity is measured. IC₅₀ values are determined from displacement curves.
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| Cell Assay |
In vitro cellular assays for fantofarone involve treating isolated cardiac myocytes or cells expressing L-type calcium channels with the compound and measuring calcium channel activity using patch-clamp electrophysiology. Whole-cell voltage-clamp recordings are performed to assess the inhibition of calcium currents. Cells are depolarized to various test potentials in the presence of increasing concentrations of fantofarone. The reduction in peak calcium current amplitude is quantified.
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| Animal Protocol |
In vivo animal experiments with fantofarone are conducted in rodent and canine models of cardiovascular disease. Animals are treated with fantofarone via oral or intravenous administration, and hemodynamic parameters such as blood pressure, heart rate, and cardiac output are measured. In models of arrhythmia, the compound's effects on arrhythmia induction and termination are assessed. Pharmacokinetic studies characterize absorption and distribution.
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| ADME/Pharmacokinetics |
Fantofarone has a molecular weight of 551.17 and a molecular formula of C₃₁H₃₆F₃N₃O₃S. It is a solid at room temperature with a purity of ≥98%. The compound is soluble in DMSO and other organic solvents. It is typically stored at -20°C, protected from light and moisture. Fantofarone is orally bioavailable with favorable pharmacokinetic properties for cardiovascular applications.
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| Toxicity/Toxicokinetics |
Fantofarone is a research compound for laboratory use only and is not approved for human therapeutic use. In preclinical studies, it has been generally well-tolerated at therapeutic doses. As a calcium channel blocker, it may cause hypotension and negative inotropic effects. Standard laboratory safety precautions should be followed when handling the compound.
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| References |
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| Additional Infomation |
Fantofarone (SR-33557; CAS 114432-13-2) is a potent, non-competitive L-type calcium channel antagonist. It has been studied for its cardiovascular effects and potential anti-arrhythmic properties. Fantofarone binds to a site distinct from the dihydropyridine site on the calcium channel. The compound is available from various commercial suppliers for research applications.
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| Molecular Formula |
C31H38N2O5S
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|---|---|
| Molecular Weight |
550.714
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| Exact Mass |
550.25
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| CAS # |
114432-13-2
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| PubChem CID |
119349
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.16g/cm3
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| Index of Refraction |
1.573
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| LogP |
6.936
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
13
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| Heavy Atom Count |
39
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| Complexity |
825
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
ITAMRBIZWGDOHW-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C31H38N2O5S/c1-23(2)27-22-33-18-7-6-9-28(33)31(27)39(34,35)26-13-11-25(12-14-26)38-20-8-17-32(3)19-16-24-10-15-29(36-4)30(21-24)37-5/h6-7,9-15,18,21-23H,8,16-17,19-20H2,1-5H3
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| Chemical Name |
N-[2-(3,4-dimethoxyphenyl)ethyl]-N-methyl-3-[4-(2-propan-2-ylindolizin-1-yl)sulfonylphenoxy]propan-1-amine
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| Synonyms |
SR33557; SR-33557; SR 33557
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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 |
| 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 (~181.58 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.54 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 (4.54 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8158 mL | 9.0792 mL | 18.1584 mL | |
| 5 mM | 0.3632 mL | 1.8158 mL | 3.6317 mL | |
| 10 mM | 0.1816 mL | 0.9079 mL | 1.8158 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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