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VK-II-86 is an inhibitor of store-overload-induced calcium release (SOICR) and a derivative of carvedilol (Cay-15418). 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. 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. VK-II-86 prevents hypokalaemia-induced ventricular arrhythmia in isolated Langendorff-perfused mouse hearts. Unlike the beta-adrenergic receptor antagonist carvedilol, it does not reverse isoproterenol-induced increases in heart rate or decrease resting heart rate in RyR2R4496C-expressing mice.Formal Name: 4-(9H-carbazol-4-yloxy)-1-[[2-(2-methoxyphenoxy)ethyl]amino]-2-butanol. CAS Number: 955371-84-3. Molecular Formula: C25H28N2O4. Formula Weight: 420.5. Purity: >90%. Formulation: (Request formulation change), A solid. Solubility: DMSO: Soluble. lambdamax: 244 nm. SMILES: OC(CCOC1=CC=CC2=C1C3=C(C=CC=C3)N2)CNCCOC4=C(OC)C=CC=C4. InChi Code: InChI=1S/C25H28N2O4/c1-29-22-10-4-5-11-23(22)31-16-14-26-17-18(28)13-15-30-24-12-6-9-21-25(24)19-7-2-3-8-20(19)27-21/h2-12,18,26-28H,13-17H2,1H3. InChi Key: OHYHNEODRHJYSS-UHFFFAOYSA-N.
This website uses cookies, which are necessary for the technical operation of the website and are always set. Other cookies, which increase the usability of this website, serve for direct advertising or simplify interaction with other websites and social networks, will only be used with your consent.
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