Cas No.: | 1428557-05-4 |
Chemical Name: | 5-(((1H-indazol-5-yl)oxy)methyl)-N-(4-(trifluoromethoxy)phenyl)pyrimidin-2-amine |
Synonyms: | ITP 2 |
Formula: | C19H14F3N5O2 |
M.Wt: | 401.349 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | A novel small molecule activator of Kv 11.1 (hERG) channel (216% over control at 3 uM for hERG1a activation); selectively increases test pulse currents (EC50=1.0 μM) and decreases tail currents, activates hERG1a homomeric channels primarily by causing large depolarizing shifts in the midpoint of voltage-dependent inactivation and hyperpolarizing shifts in the voltage-dependence of activation; exerts agonistic effect from extracellular side of the membrane and could activate the arrhythmia-associated trafficking-deficient LQT2 mutant G601S with 2 fold reduced potency, may be potentially useful in the development of LQT2 therapeutics. |