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Submit ReviewAzimilide dihydrochloride is a Kv11.1 (hERG) channel blocker, blocks rapidly activating and slowly activating components of delayed rectifier K+ currents (IC50 of 0.4 mM and 3 mM, respectively). Also inhibits Na+/Ca2+ exchanger in vitro. Shows inhibition of Na+ currents, L-type Ca2+ currents and other K+ currents at high concentrations.
分子量 | 530.88 |
公式 | C23H28ClN5O3.2HCl |
储存 | Store at -20°C |
纯度 | ≥97% (HPLC) |
CAS Number | 149888-94-8 |
PubChem ID | 6435819 |
InChI Key | HHPSICLSNHCSNZ-DSHYBBOZSA-N |
Smiles | CN1CCN(CC1)CCCCN2C(CN(C2=O)/N=C/C3=CC=C(C4=CC=C(C=C4)Cl)O3)=O.Cl.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 | |||
water | 26.54 | 50 |
以下数据基于产品分子量 530.88。 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 |
---|---|---|---|
0.5 mM | 3.77 mL | 18.84 mL | 37.67 mL |
2.5 mM | 0.75 mL | 3.77 mL | 7.53 mL |
5 mM | 0.38 mL | 1.88 mL | 3.77 mL |
25 mM | 0.08 mL | 0.38 mL | 0.75 mL |
参考文献是支持产品生物活性的出版物。
Watanabe and Kimura (2010) Inhibitory Effect of Azimilide on Na+/Ca2+ Exchange Current in Guinae-Pig Cardiac Myocytes. J.Pharmacol.Sci. 114 111 PMID: 20710119
Busch et al (1998) Blockade of HERG channels by the class III antiarrhythmic Azimilide: mode of action. Br.J.Pharmacol. 123 23 PMID: 9484850
Busch et al (1995) Blockade of Human IsK channels expression in Xenopus oocytes by the novel class III antiarrhythmic NE-10064. Eur.J.Pharmacol. 264 33 PMID: 7828640
Fermini et al (1995) Use-dependent effects of the class III antiarrhythmic agent NE-10064 (azimilide) on cardiac repolarisation: block of delayed rectifier potassium and L-type calcium currents. J.Cardiovasc.Pharmacol. 26 259 PMID: 7475051
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关键词: Azimilide dihydrochloride, Azimilide dihydrochloride supplier, potassium, channel, blockers, Kv11.1, hERG, blocks, Voltage-Gated, Potassium, Channels, Na+/Ca2+, Exchanger, 6318, Tocris Bioscience
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Azimilide was used to study Kv11.1 channel blocking properties. Kv11.1 channels were being studied to understand the voltage gating mechanism and how the activation and blocking of the channel is different than other Kv channels.