AP14145 hydrochloride
Based on 1 Customer Validation
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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- 純度: 98.3%
- CAS 番号: 2387505-59-9
- 分子式: C18H18ClF3N4O
- 分子量:398.81
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保管条件:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
IC50: 1.1 μM (KCa2.2) and 1.1 μM (KCa2.3)[1]
AP14145 (10 nM-30 μM) inhibits both hKCa2.2 and hKCa2.3 channel currents in a concentration-dependent fashion. AP14145 (10 μM) inhibits 50% of the hKCa1.1 current, 90% of the hKCa2.1 current and has no effect on hKCa3.1 channel. AP14145 (10 μM) increases the EC50 of Ca2+ on KCa2.3 channels from 0.36 to 1.2 μM[1].
AP14145 hydrochloride demonstrates an IC50 in whole-cell patch clamp on the human SK3 channel of 1.3 μM. AP14145 inhibits hERG (KV11.1) with an IC50 of 71.8 μM and Kir3.1/Kir3.4 (IKACh) with an IC50 of 9.3 μM and does not produce any significant effects on KV1.5 (IKur), KV7.1/KCNE1 (IKs), KV4.3/KChiP2 (Ito), and Kir2.1 (IK1) in 30 μM or on NaV1.5 (15 μM; INa) on a panel of cardiac ion channels. AP14145 (1-10 μM) produces no significant block of CaV1.2[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
AP14145 (2.5 and 5 mg/kg; bolus injections (iv)) increases the duration of the atrial effective refractory period in male sprague-dawley rats (250-350 g, 1-3 months old)[1].
AP14145 (5 mg/kg; bolus injections) has a Cmax of 8355 nmol/L, a t of 24.3 minutes in landrace pigs (12-13 weeks old, 30-35 kg gilts)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 2387505-59-9
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性状 Solid
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分子量 398.81
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分子式 C18H18ClF3N4O
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Color White to off-white
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SMILES
CC(NC1=C2C(N=C(N[C@@H](C3=CC=CC(C(F)(F)F)=C3)C)N2)=CC=C1)=O.[H]Cl
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
純度とドキュメンテーション
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データシート (274 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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取扱説明書 (2659 KB)
参考文献
[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]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
AP14145 hydrochloride 関連分類
HY-120355A 関連分類
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