1. Membrane Transporter/Ion Channel
  2. Potassium Channel
  3. Azimilide dihydrochloride

Azimilide dihydrochloride  (Synonyms: NE-10064 dihydrochloride)

目录号: HY-18600A 纯度: 98.91%
COA 产品使用指南

Azimilide (NE-10064) dihydrochloride 是抗心律失常化合物,能抑制 I(Ks) 和 I(Kr) 活性。

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Azimilide dihydrochloride Chemical Structure

Azimilide dihydrochloride Chemical Structure

CAS No. : 149888-94-8

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10 mM * 1 mL in Water ¥701
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5 mg ¥600
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10 mg ¥950
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Other Forms of Azimilide dihydrochloride:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Azimilide (NE-10064) dihydrochloride is a class III antiarrhythmic compound, inhibits I(Ks) and I(Kr) in guinea-pig cardiac myocytes and I(Ks) (minK) channels expressed in Xenopus oocytes. IC50 value: Target: in vitro: Azimilide dihydrochloride blocked HERG channels at 0.1 and 1 Hz with IC50s of 1.4 microM and 5.2 microM respectively. Azimilide dihydrochloride blockade of HERG channels expressed in Xenopus oocytes and I(Kr) in mouse AT-1 cells was decreased under conditions of high [K+]e, whereas block of slowly activating I(Ks) channels was not affected by changes in [K+]e [1]. Azimilide dihydrochloride suppressed the following currents (Kd in parenthesis): IKr (< 1 microM at -20 mV), IKs (1.8 microM at +30 mV), L-type Ca current (17.8 microM at +10 mV), and Na current (19 microM at -40 mV). Azimilide dihydrochloride was a weak blocker of the transient outward and inward rectifier currents (Kd > or = 50 microM at +50 and -140 mV, respectively). Azimilide dihydrochloride blocked IKr, IKs, and INa in a use-dependent manner. Furthermore, azimilide reduced a slowly inactivating component of Na current that might be important for maintaining the action potential plateau in canine ventricular myocytes [2]. In guinea pig ventricular myocytes, Azimilide (0.3-3 microM) dihydrochloride significantly prolonged action potential duration (APD) at 1 Hz. At 3 Hz, Azimilide (0.3-1 microM) dihydrochloride increased APD only slightly, and at 10 microM decreased APD and the plateau potential. Azimilide dihydrochloride potently blocked the rapidly activating component of the delayed rectifier, IKr (IC50 0.4 microM), and inhibited IKs (IC50 3 microM) with nearly 10-fold less potency [3]. in vivo: Azimilide (10 mg/kg intravenously, i.v.) dihydrochloride reduced (p < 0.05) the incidence (8 of 12) of PES-induced ventricular tachycardia (VT). The cycle length of induced VT was not prolonged by Azimilide (0.245 +/- 0.046 s predrug vs. 0.301 +/- 0.060 s postdrug) dihydrochloride. Azimilide dihydrochloride increased ventricular effective refractory period (VERP 166 +/- 5 ms predrug vs. 194 +/- 13 ms postdrug, p = 0.013), prolonged QTc interval (310 +/- 12 ms predrug vs. 350 +/- 16 ms postdrug, p = 0.004) and prolonged the effective refractory period (ERP) of noninfarcted myocardium (p = 0.045) [4].

Clinical Trial
分子量

530.88

Formula

C23H30Cl3N5O3

CAS 号
性状

固体

颜色

Light yellow to yellow

中文名称

阿齐利特二盐酸盐

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
细胞实验: 

H2O 中的溶解度 : 50 mg/mL (94.18 mM; 超声助溶)

DMSO 中的溶解度 : 2 mg/mL (3.77 mM; 超声助溶 (<60°C); 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.8837 mL 9.4183 mL 18.8366 mL
5 mM 0.3767 mL 1.8837 mL 3.7673 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

* 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
该产品水溶性佳,请具体参考实测 水 / PBS / Saline 中的溶解度数据。
您所需的储备液浓度超过该产品的实测溶解度,如有需要,请与 MCE 中国技术支持联系。
纯度 & 产品资料

纯度: 98.91%

参考文献

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO / H2O 1 mM 1.8837 mL 9.4183 mL 18.8366 mL 47.0916 mL
H2O 5 mM 0.3767 mL 1.8837 mL 3.7673 mL 9.4183 mL
10 mM 0.1884 mL 0.9418 mL 1.8837 mL 4.7092 mL
15 mM 0.1256 mL 0.6279 mL 1.2558 mL 3.1394 mL
20 mM 0.0942 mL 0.4709 mL 0.9418 mL 2.3546 mL
25 mM 0.0753 mL 0.3767 mL 0.7535 mL 1.8837 mL
30 mM 0.0628 mL 0.3139 mL 0.6279 mL 1.5697 mL
40 mM 0.0471 mL 0.2355 mL 0.4709 mL 1.1773 mL
50 mM 0.0377 mL 0.1884 mL 0.3767 mL 0.9418 mL
60 mM 0.0314 mL 0.1570 mL 0.3139 mL 0.7849 mL
80 mM 0.0235 mL 0.1177 mL 0.2355 mL 0.5886 mL

* 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
Azimilide dihydrochloride
目录号:
HY-18600A
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