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Chemical Structure : AP14145
Catalog No.: 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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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.
| M.Wt | 362.356 | |
| Formula | C18H17F3N4O | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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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.
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