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Fantofarone

Catalog No. T4669   CAS 114432-13-2
Synonyms: SR 33557

Fantofarone (SR 33557) is a highly potent antagonist of Calcium Channel.

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Fantofarone Chemical Structure
Fantofarone, CAS 114432-13-2
Pack Size Availability Price/USD Quantity
1 mg In stock $ 31.00
5 mg In stock $ 72.00
10 mg In stock $ 122.00
25 mg In stock $ 247.00
50 mg In stock $ 409.00
100 mg In stock $ 531.00
1 mL * 10 mM (in DMSO) In stock $ 88.00
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Purity: 98.36%
Purity: 96.13%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Fantofarone (SR 33557) is a highly potent antagonist of Calcium Channel.
In vitro Calcium channel blockers VIZ and Fantofarone (SR) exhibit modest antimalarial effects compared to chloroquine (CQ), with slightly greater efficacy against CQ-resistant parasites. Notably, Fantofarone is approximately 10 times more effective than verapamil. Isobologram analysis indicates these blockers enhance CQ sensitivity in CQ-resistant P. falciparum, with verapamil being 2 to 3 times more effective than Fantofarone in reducing CQ resistance at comparable subinhibitory concentrations.
In vivo Administration of isosorbide dinitrate (0.3 mg/kg, i.v.) or Fantofarone (50 mg/kg, i.v.) results in a decrease in both the frequency and severity of vasospasm, with Fantofarone showing the greatest efficacy in mitigating vasospasm across both distal and proximal regions. In contrast, verapamil (0.2 mg/kg, i.v.) exhibits markedly less effectiveness. While isosorbide dinitrate effectively suppresses distal arterial intraluminal volume (AIV) reduction, it does not significantly impact the decrease in proximal diameter. Conversely, Fantofarone stands out for its substantial reduction of AIV across the experiment, whereas verapamil fails to significantly affect AIV.
Animal Research Male White rabbits are used in this study (3.0-3.2 kg). All surgical procedures are performed under anaesthesia with a mixture of ketamine and xylazine. At the end of the experiments, the animals are sacrificed by a pentobarbital overdose. The proximal femoral arteries are exposed, and the isolated arterial segments are desiccated by air infusion delivered at a rate of 80 mL/min for 8 min. After desiccation is completed, the ligatures are released and flow is restored. At the day of surgery, a 2% cholesterol/6% peanut oil diet is started for 2 weeks. Before angioplasty, the animals are randomized in 4 groups of 10 animals:1. Placebo, 1 mL/kg of NaCl 0.9%, 2. Isosorbide dinitrate, 0.3 mg/kg, 3. Verapamil, 0.2 mg/kg, 4. Fantofarone, 50 mg/kg. The doses of isosorbide dinitrate, verapamil, and fantofarone are defined in a pilot experiment as the highest doses which did not show any hypotensive effect per se and are chosen very carefully according to their activity measured in other pharmacological models.
Synonyms SR 33557
Molecular Weight 550.71
Formula C31H38N2O5S
CAS No. 114432-13-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 150 mg/mL (272.38 mM), Sonication is recommended.

TargetMolReferences and Literature

1. Adovelande J, et al. Synergy between two calcium channel blockers, verapamil and fantofarone (SR33557), in reversing chloroquine resistance in Plasmodium falciparum. Biochem Pharmacol. 1998 Feb 15;55(4):433-40. 2. Dongay B, et al. Effect of fantofarone, a new Ca2+ channel antagonist, on angioplasty-induced vasospasm in an atherosclerotic rabbit model. Biochem Pharmacol. 1998 Jun 15;55(12):2047-50.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Parasitic Compound Library Membrane Protein-targeted Compound Library Inhibitor Library Metabolism Compound Library NO PAINS Compound Library Calcium Channel Compound Library Bioactive Compound Library ReFRAME Related Library Human Metabolite Library Ion Channel Inhibitor Library

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Keywords

Fantofarone 114432-13-2 Membrane transporter/Ion channel Metabolism Microbiology/Virology Parasite Calcium Channel SR 33557 Ca channels SR33557 inhibit SR-33557 Inhibitor Ca2+ channels inhibitor

 

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