ITP-2 |CAS:1428557-05-4 Probechem Biochemicals

Chemical Structure : ITP-2

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ITP-2 (ITP2, hERG activator)

货号: 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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生物&药学活性

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.

物理化学性质&存储条件

分子量	401.349
分子式	C19H14F3N5O2
外观性状	Solid
CAS No.
储存条件	固体粉末 -20 °C 12 个月; 4°C 6 个月	配置液 -80 °C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	5-(((1H-indazol-5-yl)oxy)methyl)-N-(4-(trifluoromethoxy)phenyl)pyrimidin-2-amine

参考文献

1. Sale H, et al. Br J Pharmacol. 2017 Aug;174(15):2484-2500.

ITP-2 (ITP2, hERG activator)

生物&药学活性

物理化学性质&存储条件

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ITP-2 (ITP2, hERG activator)

生物&药学活性

物理化学性质&存储条件

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