Fantofarone Chemical Properties

Melting point:

82-83°

Density 

dz 1.21 g/cm3

storage temp. 

Store at -20°C

solubility 

DMF: 10 mg/ml; DMSO: 10 mg/ml

form 

A crystalline solid

pka

8.34 ± 0.05(at 25℃)

color 

Light yellow to yellow

InChIKey

ITAMRBIZWGDOHW-UHFFFAOYSA-N

SMILES

C1(CCN(C)CCCOC2=CC=C(S(C3=C4N(C=CC=C4)C=C3C(C)C)(=O)=O)C=C2)=CC=C(OC)C(OC)=C1

Fantofarone Usage And Synthesis

Uses

Fantofarone is a highly potent Calcium Channel antagonist.

Biological Activity

Fantofarone is a potent antagonist of Calcium Channels.

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.

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.

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. DOI:10.1016/s0006-2952(97)00482-6
[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. DOI:10.1016/s0006-2952(98)00026-4

Fantofarone(114432-13-2)Related Product Information

• INDOLIZINE
• Fantofarone