AP14145 |CAS:1446770-54-2 Probechem Biochemicals

Chemical Structure : AP14145

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AP14145 (AP-14145;AP 14145)

货号: PC-35564Not For Human Use, Lab Use Only.

AP14145 (AP-14145) is a potent, selective negative allosteric modulator of KCa2.2 and KCa2.3 with equal potency (IC50=1.1±0.3 uM).

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生物&药学活性

AP14145 (AP-14145) is a potent, selective negative allosteric modulator of KCa2.2 and KCa2.3 with equal potency (IC50=1.1±0.3 uM).
AP14145 displays weak inhibition against hKCa1.1 and hKCa3.1 channels using whole cell patch clamp test (IC50~10 uM), does not affect hKCa3.1 currents.
AP14145 reverses the effect of the positive KCa2 gating modulator NS309, increases the EC50 of Ca2+ on KCa 2.3 channels from 0.36 to 1.2 uM at 10 uM.
The inhibitory effect strongly depended on two amino acids, S508 and A533 in the channel.
AP14145 concentration-dependently prolongs atrial effective refractory period (AERP) in rats, does not trigger any apparent CNS effects in mice.

物理化学性质&存储条件

分子量	362.356
分子式	C18H17F3N4O
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	(R)-N-(2-((1-(3-(trifluoromethyl)phenyl)ethyl)amino)-1H-benzo[d]imidazol-4-yl)acetamide

参考文献

1. Simó-Vicens R, et al. Br J Pharmacol. 2017 Dec;174(23):4396-4408.

2. Diness JG, et al. Circ Arrhythm Electrophysiol. 2017 Oct;10(10). pii: e005125.

AP14145 (AP-14145;AP 14145)

生物&药学活性

物理化学性质&存储条件

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AP14145 (AP-14145;AP 14145)

生物&药学活性

物理化学性质&存储条件

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