Formulation: A solid
Formal Name: 4-(9H-carbazol-4-yloxy)-1-[[2-(2-methoxyphenoxy)ethyl]amino]-2-butanol
Purity: ≥90%
Formula Markup: C25H28N2O4
Formula Weight: 420,5
Shelf life (days): 1460
CAS Number: 955371-84-3
Notes: VK-II-86 is an inhibitor of store-overload-induced calcium release (SOICR) and a derivative of carvedilol (Item No. 15418).{61991} It inhibits SOICR in HEK293 cells expressing the ryanodine receptor 2 (RyR2) R4496C (RyR2R4496C) mutation (IC50 = 16.8 µM), a mutation that results in spontaneous calcium release from the endoplasmic reticulum. VK-II-86 (1 µM) inhibits the inward-rectifier potassium channel 2.1 (Kir2.1), cardiac late sodium current (late INa), and L-type calcium current (ICa) in isolated canine cardiomyocytes and delayed-rectifier potassium current (IKr) in HEK293 cells expressing human-ether-a-go-go (hERG), also known as Kv11.1, in hypokalaemic, but not normokalaemic, conditions.{65539} It is also an antagonist of toll-like receptor 4 (TLR4; IC50 = 32.55 µM in HEK293 cells expressing the human receptor) and inhibits hyperpolarization-activated cyclic nucleotide gated potassium channel 4 (HCN4) in COS-7 cells expressing HCN4 when used at a concentration of 10 µM.{65540} VK-II-86 prevents hypokalaemia-induced ventricular arrhythmia in isolated Langendorff-perfused mouse hearts.{65539} Unlike the β-adrenergic receptor antagonist carvedilol, it does not reverse isoproterenol-induced increases in heart rate or decrease resting heart rate in RyR2R4496C-expressing mice.{65541}
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