Fantofarone

Fantofarone is a highly potent Calcium Channel antagonist.

Product information

CAS Number: 114432-13-2

Molecular Weight: 550.71

Formula: C31H38N2O5S

Chemical Name: [2-(3,4-dimethoxyphenyl)ethyl](methyl)[3-(4-{[2-(propan-2-yl)indolizin-1-yl]sulfonyl}phenoxy)propyl]amine

Smiles: CN(CCC1=CC(OC)=C(C=C1)OC)CCCOC1C=CC(=CC=1)S(=O)(=O)C1C(=CN2C=CC=CC2=1)C(C)C

InChiKey: ITAMRBIZWGDOHW-UHFFFAOYSA-N

InChi: 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

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : ≥ 100 mg/mL (181.58 mM).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

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.

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.

Products are for research use only. Not for human use.