| Size | Price | |
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| 100mg | ||
| 250mg | ||
| 500mg | ||
| 1g |
Ibutilide fumarate (formerly U-70226-E; U 70226 E; U-70226E) is a Class III antiarrhythmic agent used for the treatment of acute cardioconversion of atrial fibrillation and atrial flutter of a recent onset to sinus rhythm by induction of slow inward sodium current.
| ln Vitro |
Ibutilide is a strong inhibitor of IKr, with an EC50 value of 20 nM at +20 mV in atrial tumor myocytes (AT-1) cells [1]. It blocked IKr in cells expressing HERG+MDR1*1 to the same degree as it did in cells expressing HERG alone (IC50: 22.5 nM vs 27.4 nM). MDR1*7-expressing cells, on the other hand, demonstrated substantial 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 lengthens the cardiac repolarization time [1]. Ibutilide infusion can result in both monomorphic and polymorphic nonsustained ventricular tachycardia [3]. The three cumulative dosages of 0.01, 0.02, and 0.05 mg/kg iv are administered over a period of 10 minutes.
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| Animal Protocol |
Animal/Disease Models: 15 adult mongrel dogs, both male and female [1]
Doses: 0.01, 0.02 and 0.05 mg/kg Route of Administration: intravenous (iv) (iv)injection; injection administration. Results for each 10-minute infusion: Action potential duration (APD90) at 90% prolongation was Dramatically longer in patients with congestive heart failure (CHF) treated with ibutilide (0.01 mg/kg) compared with controls. An increase in left and right ventricular APD90 dispersion was observed in CHF at 0.01 mg/kg but not in the control group. |
| 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
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|---|---|
| Molecular Weight |
384.57644
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| CAS # |
122647-31-8
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| Related CAS # |
Ibutilide fumarate;122647-32-9
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| SMILES |
CCCCCCCN(CCCC(C1C=CC(NS(=O)(C)=O)=CC=1)O)CC
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| 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 Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6002 mL | 13.0012 mL | 26.0024 mL | |
| 5 mM | 0.5200 mL | 2.6002 mL | 5.2005 mL | |
| 10 mM | 0.2600 mL | 1.3001 mL | 2.6002 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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