AP 14145 hydrochloride

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Cat.No. 6481 - AP 14145 hydrochloride | C18H17F3N4O.HCl
Description: KCa2 channel negative allosteric modulator
Chemical Name: N-[2-[[(1R)-1-[3-(Trifluoromethyl)phenyl]ethyl]amino]-1H-benzimidazol-7-yl]acetamide hydrochloride
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature (2)

Biological Activity

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.

Technical Data

M. Wt 398.81
Formula C18H17F3N4O.HCl
Storage Store at -20°C
Purity ≥98% (HPLC)
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.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 39.88 100
ethanol 39.88 100

Preparing Stock Solutions

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

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References

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


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Citations for AP 14145 hydrochloride

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