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

Azimilide  (Synonyms: NE-10064)

目錄號: HY-18600 純度: 99.01%
COA 產品使用指南 技術支持

Azimilide(NE-10064)是抗心律失?;衔?,能抑制I(Ks)和I(Kr)活性。

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Azimilide Chemical Structure

Azimilide Chemical Structure

CAS No. : 149908-53-2

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規(guī)格 價格 是否有貨 數(shù)量
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10 mg ¥950
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Other Forms of Azimilide:

  • 生物活性

  • 純度 & 產品資料

  • 參考文獻

生物活性

Azimilide(NE-10064) 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 blocked HERG channels at 0.1 and 1 Hz with IC50s of 1.4 microM and 5.2 microM respectively. Azimilide 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 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 was a weak blocker of the transient outward and inward rectifier currents (Kd > or = 50 microM at +50 and -140 mV, respectively). Azimilide 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, NE-10064 (0.3-3 microM) significantly prolonged action potential duration (APD) at 1 Hz. At 3 Hz, NE-10064 (0.3-1 microM) increased APD only slightly, and at 10 microM decreased APD and the plateau potential. NE-10064 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: NE-10064 (10 mg/kg intravenously, i.v.) 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 NE-10064 (0.245 +/- 0.046 s predrug vs. 0.301 +/- 0.060 s postdrug). NE-10064 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

457.95

Formula

C23H28ClN5O3

CAS 號
性狀

固體

顏色

Off-white to light brown

中文名稱

阿齊利特

運輸條件

Room temperature in continental US; may vary elsewhere.

儲存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性數(shù)據
細胞實驗: 

DMSO 中的溶解度 : 125 mg/mL (272.96 mM; 超聲助溶; 吸濕的 DMSO 對產品的溶解度有顯著影響,請使用新開封的 DMSO)

配制儲備液
濃度 溶劑體積 質量 1 mg 5 mg 10 mg
1 mM 2.1836 mL 10.9182 mL 21.8364 mL
5 mM 0.4367 mL 2.1836 mL 4.3673 mL
查看完整儲備液配制表

* 請根據產品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復凍融造成的產品失效。
儲備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C儲存時,請在6個月內使用,-20°C儲存時,請在1個月內使用。

  • 摩爾計算器

  • 稀釋計算器

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

質量
=
濃度
×
體積
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動物溶解方案計算器
請輸入動物實驗的基本信息:

給藥劑量

mg/kg

動物的平均體重

g

每只動物的給藥體積

μL

動物數(shù)量

由于實驗過程有損耗,建議您多配一只動物的量
計算結果
工作液所需濃度 : mg/mL
純度 & 產品資料
參考文獻

完整儲備液配制表

* 請根據產品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復凍融造成的產品失效
儲備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C儲存時,請在6個月內使用,-20°C儲存時,請在1個月內使用。

可選溶劑 濃度 溶劑體積 質量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1836 mL 10.9182 mL 21.8364 mL 54.5911 mL
5 mM 0.4367 mL 2.1836 mL 4.3673 mL 10.9182 mL
10 mM 0.2184 mL 1.0918 mL 2.1836 mL 5.4591 mL
15 mM 0.1456 mL 0.7279 mL 1.4558 mL 3.6394 mL
20 mM 0.1092 mL 0.5459 mL 1.0918 mL 2.7296 mL
25 mM 0.0873 mL 0.4367 mL 0.8735 mL 2.1836 mL
30 mM 0.0728 mL 0.3639 mL 0.7279 mL 1.8197 mL
40 mM 0.0546 mL 0.2730 mL 0.5459 mL 1.3648 mL
50 mM 0.0437 mL 0.2184 mL 0.4367 mL 1.0918 mL
60 mM 0.0364 mL 0.1820 mL 0.3639 mL 0.9099 mL
80 mM 0.0273 mL 0.1365 mL 0.2730 mL 0.6824 mL
100 mM 0.0218 mL 0.1092 mL 0.2184 mL 0.5459 mL
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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產品名稱:
Azimilide
目錄號:
HY-18600
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