Hesperadin是ATP竞争性Aurora B抑制剂,IC50为250 nM。
Hesperadin potently inhibits Aurora B with IC50 of 250 nM in a cell-free assay. It markedly reduces the activity of AMPK, Lck, MKK1, MAPKAP-K1, CHK1 and PHK while it does not inhibit MKK1 activity in vivo.
500 nM 左右
动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数 | |
例如,已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法:将88 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到该药物用于大鼠的等效剂量44 mg/kg。
[1] Hauf S, et al. J Cell Biol, 2003, 161(2), 281-294.
分子式 C29H32N4O3S |
分子量 516.65 |
CAS号 422513-13-1 |
储存方式 ﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂(常温) |
DMSO ≥100 mg/mL |
Water <1 mg/mL |
Ethanol <1 mg/mL |
体内溶解度
NCT Number | Conditions | Interventions | Sponsor/Collaborators | Phases | Start Date | Last Updated |
NCT02365532 | Long QT Syndrome | Drug: GS-6615|Drug: Placebo to match GS-6615|Drug: Placebo to match dofetilide|Drug: Dofetilide | Gilead Sciences | Phase 1 | 2015-02-01 | 2015-05-19 |
NCT01877486 | Paroxysmal Atrial Fibrillation|Persistent Atrial Fibrillation | Procedure: Ablation | University of Rochester|Medtronic | Phase 4 | 2016-01-01 | 2016-10-02 |
NCT02439658 | Long QT Syndrome|Drug Toxicity | Drug: Dofetilide and/or sotalol | Massachusetts General Hospital|VA Office of Research and Development|Beth Israel Deaconess Medical Center|Brigham and Women's Hospital | 2014-01-01 | 2016-03-27 | |
NCT02308748 | Drug-induced QT Prolongation|Pharmacokinetics|Pharmacodynamics | Drug: Dofetilide|Drug: Mexiletine|Drug: Lidocaine|Drug: Moxifloxacin|Drug: Diltiazem|Drug: Placebo | Food and Drug Administration (FDA)|Spaulding Clinical Research LLC | Phase 1 | 2014-05-01 | 2016-06-06 |
NCT01873950 | Drug-induced Surface ECG Changes | Drug: Ranolazine|Drug: Dofetilide|Drug: Verapamil|Drug: Quinidine sulfate|Drug: Placebo | Food and Drug Administration (FDA)|Spaulding Clinical Research LLC | Phase 1 | 2013-05-01 | 2015-12-14 |
NCT02241252 | Cardiac Arrhythmia|Qt Interval, Variation in | Device: iPhone ECG | University of Oklahoma | 2013-09-01 | 2015-05-28 | |
NCT03070470 | Drug-induced QT Prolongation|Pharmacokinetics|Pharmacodynamics | Drug: Ranolazine|Drug: Verapamil|Drug: Lopinavir / Ritonavir|Drug: Chloroquine|Drug: Placebo|Drug: Dofetilide and Diltiazem | Food and Drug Administration (FDA)|Spaulding Clinical Research LLC | Phase 1 | 2017-03-14 | 2017-03-18 |
NCT01505296 | Atrial Fibrillation | Drug: Antiarrhythmic drug|Procedure: Catheter ablation | Valley Health System|Biosense Webster, Inc. | Phase 4 | 2011-12-01 | 2014-12-13 |
NCT00408200 | Atrial Fibrillation | Drug: propafenone; flecainide; sotalol; dofetilide|Device: Radiofrequency catheter ablation | University of Pennsylvania | 2006-11-01 | 2013-01-31 | |
NCT00540787 | Paroxysmal Atrial Fibrillation | Device: Radiofrequency ablation, antiarrhythmic drugs|Drug: Amiodarone, flecainide, propafenone, quinidine, dofetilide, sotalol, cibenzoline, beta blocking and calcium channel blocking agents and antiarrhythmic drugs|Device: ThermoCool Radiofrequency Catheter | Biosense Webster, Inc. | Phase 4 | 2003-08-01 | 2012-02-21 |
NCT00392106 | Atrial Fibrillation | Drug: propafenone|Drug: flecainide|Drug: dofetilide|Drug: sotolol|Device: Pulmonary vein ablation|Drug: Amiodarone | ProRhythm, Inc. | Phase 3 | 2006-04-01 | 2008-06-16 |
NCT02214069 | Atrial Fibrillation|Atrial Flutter | Device: Record and transmit heart rhythm | The Cleveland Clinic|AliveCor | 2014-08-01 | 2017-01-24 | |
NCT00589303 | Atrial Fibrillation|Heart Failure | Drug: FDA approved rate and rhythm control drugs|Device: AV Node ablation and device implant | Mayo Clinic|Medtronic | Phase 3 | 2007-12-01 | 2013-02-25 |
NCT01877473 | Persistent Atrial Fibrillation | Procedure: Ablation | Valley Health System | Phase 4 | 2013-05-01 | 2014-06-16 |
NCT01097330 | Defibrillators, Implantable|Tachycardia, Ventricular | Procedure: Ablation|Drug: Amiodarone | Population Health Research Institute|St. Jude Medical|Hamilton Health Sciences Corporation | Phase 3 | 2010-08-01 | 2011-08-04 |
NCT00911508 | Atrial Fibrillation|Arrhythmia | Device: Left atrial ablation|Drug: Rate or Rhythm Control Therapy | Mayo Clinic|National Heart, Lung, and Blood Institute (NHLBI)|St. Jude Medical|Biosense Webster, Inc. | 2009-08-01 | 2016-04-25 | |
NCT00578617 | Atrial Fibrillation|Arrhythmia | Drug: Rate Control|Device: Ablation Therapy|Drug: Rate Control|Drug: Rate control|Drug: Rate control|Drug: Rate control|Drug: Rate Control|Drug: Rate Control|Drug: Rate Control|Drug: Rhythm Control|Drug: Rhythm control|Drug: Rhythm control|Drug: Rhythm control|Drug: Rhythm control|Drug: Rhythm control | Mayo Clinic|Duke Clinical Research Institute|St. Jude Medical | 2006-09-01 | 2012-12-03 |
注:以上所有数据均来自公开文献,并不保证对所有实验均有效,数据仅供参考。
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