Fantofarone (Synonyms: SR 33557) |
| Catalog No.GC19152 |
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Cas No.: 114432-13-2
Sample solution is provided at 25 µL, 10mM.
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Fantofarone is a highly potent Calcium Channel antagonist.
It can be seen that the calcium channel blockers VIZ and Fantofarone (SR) possess a weak intrinsic antimalarial property compared to CQ, and both appear slightly more potent on the CQ-resistant than on the CQ-sensitive parasites. Interestingly, Fantofarone is ca. 10 times more potent than verapamil. Fantofarone (SR) is 10 times more potent than the phenylalkylamine verapamil (VR) on the two P. fdciparum strains. As revealed by the isobolograms, the two calcium channel blockers potentiate the CQ sensitivity activity on the CQ-resistant P. fufcipurum strain, verapamil appearing 2 to 3 times more potent than Fantofarone. Furthermore, when used at similar subinhibitory fractions of their IC50, VR is 2 to 3 times more potent than Fantofarone in decreasing CQ resistance[1].
Treatment with isosorbide dinitrate (0.3 mg/kg, i.v.) or Fantofarone (50 mg/kg, i.v.), a reduction is observed in the occurrence and severity of vasospasm, whereas verapamil (0.2 mg/kg, i.v.) is much less effective. Although it totally inhibits distal AIV, isosorbide dinitrate does not significantly affect proximal diameter decrease. The most potent compound with regard to both the distal and proximal vasospasms is Fantofarone, which significantly reduces AIV throughout the experiment. Verapamil does not reduce AIV significantly[2].
References:
[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.
Animal experiment: | Rabbits[2]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[2]. |
References: [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. | |
| Cas No. | 114432-13-2 | SDF | |
| Synonyms | SR 33557 | ||
| Canonical SMILES | O=S(C1=C2N(C=CC=C2)C=C1C(C)C)(C3=CC=C(OCCCN(C)CCC4=CC(OC)=C(OC)C=C4)C=C3)=O | ||
| Formula | C31H38N2O5S | M.Wt | 550.71 |
| Solubility | DMSO : 150 mg/mL (272.38 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
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 |
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- Purity: >99.50%
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Average Rating: 5 (Based on Reviews and 22 reference(s) in Google Scholar.)
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