2387505-59-9
Chemical Structure
AP14145 hydrochloride
- CAS No.: 2387505-59-9
- Formula:C18H18ClF3N4O
- Molecular Weight:398.81
IUPAC Name: (R)-N-(2-((1-(3-(trifluoromethyl)phenyl)ethyl)amino)-1H-benzo[d]imidazol-7-yl)acetamide hydrochloride
InChIKey: KGIUXIYNTCVBST-HNCPQSOCSA-N
SMILES: CC(NC1=C2C(N=C(N[C@@H](C3=CC=CC(C(F)(F)F)=C3)C)N2)=CC=C1)=O.[H]Cl
Biological Activity: AP14145 hydrochloride is a potent KCa2 (SK) channel negative allosteric modulator with an IC50 of 1.1 μM for KCa2.2 (SK2) and KCa2.3 (SK3) channels. AP14145 hydrochloride inhibition strongly depends on two amino acids, S508 and A533 in the channel. AP14145 hydrochloride prolonged atrial effective refractory period (AERP) in rats and demonstrates antiarrhythmic effects in a Vernakalant-resistant porcine model of atrial fibrillation (AF)[1][2].
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AP14145 hydrochloride | 98.3% | AP14145 hydrochloride is a potent KCa2 (SK) channel negative allosteric modulator with an IC50 of 1.1 μM for KCa2.2 (SK2) and KCa2.3 (SK3) channels. AP14145 hydrochloride inhibition strongly depends on two amino acids, S508 and A533 in the channel. AP14145 hydrochloride prolonged atrial effective refractory period (AERP) in rats and demonstrates antiarrhythmic effects in a Vernakalant-resistant porcine model of atrial fibrillation (AF). | ||||||||||||||||||||
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- [1]. Rafel Simó-Vicens, et al. A New Negative Allosteric Modulator, AP14145, for the Study of Small Conductance Calcium-Activated Potassium (KCa2) Channels. Br J Pharmacol. 2017 Dec;174(23):4396-4408. [Content Brief]
- [2]. Jonas Goldin Diness, et al. Termination of Vernakalant-Resistant Atrial Fibrillation by Inhibition of Small-Conductance Ca2+-Activated K + Channels in Pigs. Circ Arrhythm Electrophysiol. 2017 Oct;10(10):e005125. [Content Brief]
Keywords
