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Submit ReviewAP 14145 hydrochloride is a KCa2 (small conductance Ca2+-activated potassium) channel negative allosteric modulator (IC50 = 1.1 μM). Increases the EC50 of Ca2+ on KCa2.3 channels by ~3-fold. Prolongs atrial effective refractory period (AERP) in rats. Reduces atrial fibrillation (AF) duration and prolongs atrial refractoriness without affecting ventricular refractory period in an animal AF model.
M. Wt | 398.81 |
Formula | C18H17F3N4O.HCl |
Storage | Store at -20°C |
Purity | ≥98% (HPLC) |
CAS Number | 2387505-59-9 |
InChI Key | KGIUXIYNTCVBST-HNCPQSOCSA-N |
Smiles | C[C@H](C1=CC(C(F)(F)F)=CC=C1)NC2=NC3=CC=CC(NC(C)=O)=C3N2.Cl |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 39.88 | 100 | |
ethanol | 39.88 | 100 |
The following data is based on the product molecular weight 398.81. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 2.51 mL | 12.54 mL | 25.07 mL |
5 mM | 0.5 mL | 2.51 mL | 5.01 mL |
10 mM | 0.25 mL | 1.25 mL | 2.51 mL |
50 mM | 0.05 mL | 0.25 mL | 0.5 mL |
References are publications that support the biological activity of the product.
Diness et al (2017) Termination of vernakalant-resistant atrial fibrillation by inhibition of small-conductance Ca2+-activated K+ channels in pigs. Circ.Arrhythm.Electrophysiol. 10 e005125 PMID: 29018164
Simó-Vicens et al (2017) A new negative allosteric modulator, AP14145, for the study of small conductance calcium-activated potassium (KCa2) channels. Br.J.Pharmacol. 174 4396 PMID: 28925012
If you know of a relevant reference for AP 14145 hydrochloride, please let us know.
View all Calcium-Activated Potassium (KCa) Channel Modulators
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