Fantofarone

Fantofarone is a calcium channel inhibitor. It selectively inhibits the L-type voltage-gated calcium channel in isolated rat aorta (IC50 = 0.61 nM) over alpha1- and beta-adrenergic, muscarinic, and histamine H2 receptors in rat heart homogenates (IC50s = >10, 4, >10, and >10 µM, respectively), and the serotonin receptor subtypes 5-HT1 and 5-HT2, as well as histamine H1 and adenosine A1 receptors, in rat brain homogenates (IC50s = >10, >10, 4, and >10 µM, respectively). Fantofarone inhibits peak calcium current in depolarized and hyperpolarized L-type voltage-gated calcium channels (IC50s = 1.4 and 150 nM, respectively). It inhibits potassium chloride- and norepinephrine-induced contractions in isolated rat aorta (IC50s = 5.64 and 96 nM, respectively). It enhances recovery of cardiac output during reperfusion of isolated rat hearts when used at a concentration of 10 nM. Fantofarone prevents angioplasty-induced vasospasms in the femoral artery in a rabbit model of focal atherosclerosis when administered at a dose of 50 µg/kg.Formal Name: 3,4-dimethoxy-N-methyl-N-[3-[4-[[2-(1-methylethyl)-1-indolizinyl]sulfonyl]phenoxy]propyl]-benzeneethanamine. CAS Number: 114432-13-2. Synonyms: SR 33557. Molecular Formula: C31H38N2O5S. Formula Weight: 550.7. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 10 mg/ml, DMSO: 10 mg/ml. lambdamax: 233, 304 nm. SMILES: COC1=CC=C(CCN(C)CCCOC2=CC=C(S(C3=C4N(C=CC=C4)C=C3C(C)C)(=O)=O)C=C2)C=C1OC. InChi Code: 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. InChi Key: ITAMRBIZWGDOHW-UHFFFAOYSA-N.