A calcium channel inhibitor; inhibits the L-type voltage-gated calcium channel in isolated rat aorta (IC50 = 0.61 nM) over α1- and β-adrenergic

Fantofarone – 10 mg

Brand:
Cayman
CAS:
114432-13-2
Storage:
-20
UN-No:
Non-Hazardous - /

Fantofarone is a calcium channel inhibitor.{47567} It selectively inhibits the L-type voltage-gated calcium channel in isolated rat aorta (IC50 = 0.61 nM) over α1- and β-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).{47568} It inhibits potassium chloride- and norepinephrine-induced contractions in isolated rat aorta (IC50s = 5.64 and 96 nM, respectively).{47567} It enhances recovery of cardiac output during reperfusion of isolated rat hearts when used at a concentration of 10 nM.{47569} 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.{47570}  

 

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SKU: 26381 - 10 mg Category:

Description

A calcium channel inhibitor; inhibits the L-type voltage-gated calcium channel in isolated rat aorta (IC50 = 0.61 nM) over α1- and β-adrenergic, muscarinic, and histamine H2 receptors in rat heart homogenates (IC50s = >10, >10, 4, 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, 4, >10, and >10 µM, respectively); inhibits peak calcium current in depolarized and hyperpolarized L-type voltage-gated calcium channels (IC50s = 1.4 and 150 nM, respectively); inhibits potassium chloride- and norepinephrine-induced contractions in isolated rat aorta (IC50s = 5.64 and 96 nM, respectively); enhances recovery of cardiac output during reperfusion of isolated rat hearts at 10 nM; prevents angioplasty-induced vasospasms in the femoral artery in a rabbit model of focal atherosclerosis at 50 µg/kg

Formal name: 3,4-dimethoxy-N-methyl-N-[3-[4-[[2-(1-methylethyl)-1-indolizinyl]sulfonyl]phenoxy]propyl]-benzeneethanamine

Synonyms:  SR 33557

Molecular weight: 550.7

CAS: 114432-13-2

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Ion Channel Modulation|Blockers||Research Area|Cardiovascular System|Cardiovascular Diseases|Atherosclerosis||Research Area|Cardiovascular System|Heart||Research Area|Cardiovascular System|Vasculature|Vasodilation||Research Area|Cell Biology|Cell Signaling|Calcium Mobilization

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