Fantofarone

SKU: orb1222852

Description

Fantofarone, also known as SR 33557, is a highly potent calcium channel antagonist representative of a new class of slow channel blockers. Fantofarone can significantly modify cardiac function and in particular, decrease MO2C consumption during periods of elevated heart rate. Fantofarone is able to induce submaximal peripheral vasodilating effects at doses that are devoid of any clinically significant cardiac effect.

Key Properties

• CAS Number: 114432-13-2
• MW: 550.72
• Purity: >98% (HPLC)
• Formula: C₃₁H₃₈N₂O₅S
• SMILES: COc1ccc(cc1OC)CCN(C)CCCOc2ccc(cc2)S(=O)(=O)c3c4ccccn4cc3C(C)C
• Target: Calcium Channel
• Solubility: DMSO : 150 mg/mL 272.38 mM

Bioactivity

• In Vivo:
  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.
• In Vitro:
  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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

SR 33557 | SR-33557 | Fantofarone

Quick Database Links

Gene Symbol

Calcium Channel