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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.
分子量 | 398.81 |
公式 | C18H17F3N4O.HCl |
储存 | Store at -20°C |
纯度 | ≥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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 39.88 | 100 | |
ethanol | 39.88 | 100 |
以下数据基于产品分子量 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.
浓度/溶剂体积/质量 | 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 |
参考文献是支持产品生物活性的出版物。
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.
关键词: AP 14145 hydrochloride, AP 14145 hydrochloride supplier, 1446770-54-2, AP14145, hydrochloride, KCa2, calcium, activated, potassium, channels, negative, allosteric, modulators, modulates, NAM, atrial, effective, refractory, period, AERP, fibrillation, Kca2.2, kca2.3, Ca2+-Activated, Potassium, Channels, 6481, Tocris Bioscience
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