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Purity: ≥98%
Ibutilide fumarate (formerly known as U 70226 E; U-70226-E; U-70226E), the fumarate salt of Ibutilide, is a Class III antiarrhythmic agent that has been used for treating acute cardioconversion of atrial fibrillation and atrial flutter of a recent onset to sinus rhythm by induction of slow inward sodium current. Ibutilide Fumarate acts as a sodium channel protein inhibitor and methanesulfonanilide anti-arrhythmic agent that prolongs myocardial action potential duration mostly by activation of slow inward sodium current.
| ln Vitro |
Ibutilide fumarate is a strong IKr blocker with an EC50 value of 20 nM at +20 mV in atrial tumor myocytes (AT-1) cells[1]. Ibutilide fumarate suppresses IKr in cells expressing HERG+MDR1*1 to the same extent as cells expressing HERG alone (IC50: 22.5 nM vs 27.4 nM). However, cells expressing MDR1*7 demonstrate a considerable resistance to Ibutilide (IC50: 105.3 nM vs 27.4 nM)[2].
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| ln Vivo |
Both in vivo and in vitro, ibutilide fumarate prolongs cardiac repolarization[1]. When ibutilide fumarate is given in three cumulative doses of 0.01, 0.02 and 0.05 mg/kg iv, each given as a 10-min infusion, both polymorphic and monomorphic non-sustained ventricular tachycardia are produced[3].
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| Animal Protocol |
Animal/Disease Models: Fifteen adult mongrel dogs of either sex[1]
Doses: 0.01, 0.02 and 0.05 mg/kg Route of Administration: intravenous (iv) injection; each as a 10-min infusion Experimental Results: The action potential duration at 90% (APD90) prolongation with Ibutilide (0.01 mg/kg) was Dramatically greater in congestive heart failure (CHF) vs. controls. An increased dispersion of left-right ventricular APD90 was observed in CHF at 0.01 mg/kg, but not in controls. |
| References |
[1]. Ibutilide, a methanesulfonanilide antiarrhythmic, is a potent blocker of the rapidly activating delayed rectifier K+ current (IKr) in AT-1 cells. Concentration-, time-, voltage-, and use-dependent effects. Circulation. 1995 Mar 15;91(6):1799-806.
[2]. B F McBride, et al. Influence of the G2677T/C3435T haplotype of MDR1 on P-glycoprotein trafficking and Ibutilide-induced block of HERG. Pharmacogenomics J. 2009 Jun;9(3):194-201. [3]. S S Chugh, et al. Altered response to Ibutilide in a heart failure model. Cardiovasc Res. 2001 Jan;49(1):94-102. |
| Molecular Formula |
(C20H36N2O3S)2.C4H4O4
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| Molecular Weight |
885.23
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| CAS # |
122647-32-9
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| Related CAS # |
Ibutilide;122647-31-8;Ibutilide-d5 fumarate
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| SMILES |
S(C([H])([H])[H])(N([H])C1C([H])=C([H])C(=C([H])C=1[H])C([H])(C([H])([H])C([H])([H])C([H])([H])N(C([H])([H])C([H])([H])[H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H])O[H])(=O)=O.S(C([H])([H])[H])(N([H])C1C([H])=C([H])C(=C([H])C=1[H])C([H])(C([H])([H])C([H])([H])C([H])([H])N(C([H])([H])C([H])([H])[H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H])O[H])(=O)=O.O([H])C(/C(/[H])=C(\[H])/C(=O)O[H])=O
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| InChi Key |
ALOBUEHUHMBRLE-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H36N2O3S/c1-4-6-7-8-9-16-22(5-2)17-10-11-20(23)18-12-14-19(15-13-18)21-26(3,24)25/h12-15,20-21,23H,4-11,16-17H2,1-3H3
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| Chemical Name |
N-[4-[4-[ethyl(heptyl)amino]-1-hydroxybutyl]phenyl]methanesulfonamide
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.1296 mL | 5.6482 mL | 11.2965 mL | |
| 5 mM | 0.2259 mL | 1.1296 mL | 2.2593 mL | |
| 10 mM | 0.1130 mL | 0.5648 mL | 1.1296 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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