| 產(chǎn)品描述： | Ibutilide (U70226E) fumarate, an action potential-prolonging antiarrhythmic, is a potent blocker of the rapidly activating delayed rectifier K+ current (IKr) in AT-1 cells |
| 靶點(diǎn)： |
Potassium Channel;CalciumChannel;?SodiumChannel |
| 體外研究： |
Ibutilide fumarate is a potent IKr blocker with an EC50 value of 20 nM at +20 mV in atrial tumor myocytes (AT-1) cells. Ibutilide fumarate blocks 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 show a marked resistance to Ibutilide (IC50: 105.3 nM vs 27.4 nM) |
| 體內(nèi)研究： |
Ibutilide fumarate prolongs cardiac repolarization in vitro and in vivo. Ibutilide (administered cumulatively in three doses, 0.01, 0.02 and 0.05 mg/kg i.v., each as a 10-min infusion) fumarate results in both polymorphic and monomorphic non-sustained ventricular tachycardia. Animal Model: Fifteen adult mongrel dogs of either sex Dosage: 0.01, 0.02 and 0.05 mg/kg Administration: Intravenous injection; each as a 10-min infusion Result: The action potential duration at 90% (APD90) prolongation with Ibutilide (0.01 mg/kg) was significantly 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. |
| 參考文獻(xiàn)： |
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. |
| 溶解性： |
Soluble in DMSO、H2O |
| 保存條件： |
2-8℃ |
| 配置溶液濃度參考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.259 ml |
11.297 ml |
22.593 ml |
| 5 mM |
0.452 ml |
2.259 ml |
4.519 ml |
| 10 mM |
0.226 ml |
1.13 ml |
2.259 ml |
| 50 mM |
0.045 ml |
0.226 ml |
0.452 ml |
|
| 注意： |
部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。 |
上海工商
危險(xiǎn)品化學(xué)品經(jīng)營(yíng)許可證（不帶存儲(chǔ)）
營(yíng)業(yè)執(zhí)照(三證合一)
掃一掃關(guān)注上海源葉微信公眾號(hào)
北京