决奈达隆盐酸盐, 电压门 L 型钙通道阻滞剂

Calcium Channel Inhibitors
  • 10mM in DMSO
有货

库存信息

关闭
货号 (SKU) 包装规格 是否现货 价格 数量
D408521-1ml
1ml 现货 Stock Image
查看相关系列
Compound libraries (12332)

基本描述

英文别名 SR33589 | N-​[2-​butyl-​3-​[4-​[3-​(dibutylamino)​propoxy]​benzoyl]​-​5-​benzofuranyl]​-methanesulfonamide,hydrochloride (1:1)
规格或纯度 10mM in DMSO
英文名称 Dronedarone HCl
生化机理 盐酸决奈达隆(SR33589)是一种针对钾通道、钠通道和钙通道的多通道阻滞剂,是治疗心房颤动(房颤)的抗心律失常药物。
储存温度 -80℃储存
运输条件 超低温冰袋运输
作用类型 封闭剂
作用机制 电压门 L 型钙通道阻滞剂
产品介绍


Information

Dronedarone HCl Dronedarone HCl (SR33589) is a multichannel blocker targeting potassium channel , sodium channel and calcium channel , used as an antiarrhythmic drug for treatment of atrial fibrillation (AF).
In vitro

Dronedarone reduces the incidence of early and delayed after depolarizations evoked by 1 mM Dofetilide and 0.2 mM Strophantidine in Purkinje fibres. Dronedarone (10 mM) markedly reduces the L-type calcium current (76.5%) and the rapid component of the delayed rectifier potassium current (97%) in ventricular myocytes. Dronedarone inhibits the activity of I(K(ACh)) channels recorded from cell-attached patches by reducing the channel open probability (from 0.56 to 0.11) without modification of the single-channel conductance in single cells isolated from sinoatrial node (SAN) tissue of rabbit hearts. Dronedarone exhibits a state-dependent inhibition of the fast Na(+) channel current with an IC50 of 0.7 μM in guinea pig ventricular myocytes, when the holding potential (V (hold)) is -80 mV. Dronedarone blocks Ca(2+) currents elicited by rectangular pulses at V (hold)\u2009=\u2009-40 mV with IC50 value of 0.4 μM, whereas at V (hold)\u2009=\u2009-80 mV, Dronedarone (10 μM) blocks only 20\u2009% of the current.

In vivo

Dronedarone increases action potential duration in normal hearts of rats. Dronedarone reduces the late sustained K(+) current, I(K) (or Isus) by 69%. Dronedarone induces only a tonic block of I(K). Dronedarone induces a weak increase in the fast transient outward current, I(to), in rats after myocardial infarction.
Cell Data

cell lines:Human breast cancer cells MDA-MB-468

Concentrations:

Incubation Time:

Powder Purity:≥99%

产品属性

ALogP 7.397
hba_count 5
HBD Count 1
Rotatable Bond 18

关联靶点(人)

KCNA5 Tclin 钾电压门控通道亚家族 A 成员 5(Potassium voltage-gated channel subfamily A member 5) (1 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)

名称和识别符

分子类型 小分子
Canonical SMILES Cl.CCCCN(CCCC)CCCOC1=CC=C(C=C1)C(=O)C2=C(CCCC)OC3=CC=C(N[S](C)(=O)=O)C=C23
分子量 593.22
Reaxy-Rn 8380427
Reaxys-RN link address https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=8380427&ln=

化学和物理性质

DMSO(mg / mL) Max Solubility 80
DMSO(mM) Max Solubility 134.86
Water(mg / mL) Max Solubility <1

安全和危险性(GHS)

Reaxy-Rn 8380427
Reaxys-RN link address https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=8380427&ln=

技术规格说明书

Concentration(Compounding value) 9-11(mmol/L)
Record the entire process by video Conform

质检证书(CoA,COO,BSE/TSE 和分析图谱)

C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:

溶液计算器

Shall we send you a message when we have discounts available?

Remind me later

Thank you! Please check your email inbox to confirm.

Oops! Notifications are disabled.