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Chemical Structure : ITP-2
Catalog No.: PC-60831Not For Human Use, Lab Use Only.
ITP-2 is a novel small molecule activator of Kv11.1 (hERG) channel (216% over control at 3 uM for hERG1a activation).
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ITP-2 is a novel small molecule activator of Kv11.1 (hERG) channel (216% over control at 3 uM for hERG1a activation).
ITP-2 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.
ITP-2 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.
| M.Wt | 401.349 | |
| Formula | C19H14F3N5O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Sale H, et al. Br J Pharmacol. 2017 Aug;174(15):2484-2500.
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