2. Membrane Transporter/Ion Channel
  3. Potassium Channel
  4. AVE-0118

AVE-0118 is a Kv1.5 potassium channel blocker and antiarrhythmic agent. AVE-0118 blocks neuronal Kv1.5 potassium channels, thereby enhancing the release of norepinephrine. AVE-0118 enhances field stimulation-induced neurogenic contraction, an effect sensitive to α1-adrenergic receptor blockade. AVE-0118 terminates persistent atrial fibrillation in some dogs. AVE-0118 is applicable to research related to atrial fibrillation and persistent atrial fibrillation.

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AVE-0118

AVE-0118 構造式

CAS 番号 : 498577-53-0

容量 価格（税別） 在庫状況 数量
1 mg $114 在庫あり
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Based on 1 publication(s) in Google Scholar

AVE-0118 関連抗体

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製品説明

AVE-0118 is a Kv1.5 potassium channel blocker and antiarrhythmic agent. AVE-0118 blocks neuronal Kv1.5 potassium channels, thereby enhancing the release of norepinephrine. AVE-0118 enhances field stimulation-induced neurogenic contraction, an effect sensitive to α1-adrenergic receptor blockade. AVE-0118 terminates persistent atrial fibrillation in some dogs. AVE-0118 is applicable to research related to atrial fibrillation and persistent atrial fibrillation[1][2].

IC50 & Target[1]

Kv1.5

 

体外実験

AVE-0118 (0.1 μM; 20 min) does not alter basal tone or noradrenaline-induced contractions in isolated third- or fourth-order rat small mesenteric artery ring segments[1].
AVE-0118 (0.1 μM; 20 min) significantly potentiates electrical field stimulation-induced neurogenic contractions in isolated third- or fourth-order rat small mesenteric artery ring segments, increasing the 16 Hz EFS response from 19.7% to 44.9% of maximum phenylephrine-induced tone[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

AVE-0118 関連抗体
体内実験

AVE-0118 (6 mg/kg; i.v.; single dose) terminates persistent atrial fibrillation in 43% of treated beagle dogs with AF-induced atrial remodeling, with sustained sinus rhythm maintained in 29% of animals[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Beagle (chronic atrioventricular block, persistent atrial fibrillation induced by left atrial tachypacing)[2]
Dosage: 6 mg/kg
Administration: i.v.; infused over 10 minutes
Result: Terminated persistent AF in 3 out of 7 animals, at 12 minutes, 12.4 hours, and 16 minutes after administration start.
Resulted in a cardioversion rate of 43% (3/7).
Maintained sustained sinus rhythm (no recurrence) in 29% (2/7) of animals.
Saw AF recurrence in 1 of the 3 successfully cardioverted animals at 34 minutes after AF termination.
分子量

479.57

分子式

C30H29N3O3
CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

O=C(NCCC1=CC=CN=C1)C2=CC=CC=C2C3=CC=CC=C3CNC(CC4=CC=C(C=C4)OC)=O
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : 100 mg/mL (208.52 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0852 mL 10.4260 mL 20.8520 mL
5 mM 0.4170 mL 2.0852 mL 4.1704 mL
10 mM 0.2085 mL 1.0426 mL 2.0852 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Concentration
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Volume
×
Molecular Weight *

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

C1

×
体積 （開始）

V1

=
濃度 （終了）

C2

×
体積 （終了）

V2

体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (5.21 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (5.21 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション
参考文献

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0852 mL 10.4260 mL 20.8520 mL 52.1300 mL
5 mM 0.4170 mL 2.0852 mL 4.1704 mL 10.4260 mL
10 mM 0.2085 mL 1.0426 mL 2.0852 mL 5.2130 mL
15 mM 0.1390 mL 0.6951 mL 1.3901 mL 3.4753 mL
20 mM 0.1043 mL 0.5213 mL 1.0426 mL 2.6065 mL
25 mM 0.0834 mL 0.4170 mL 0.8341 mL 2.0852 mL
30 mM 0.0695 mL 0.3475 mL 0.6951 mL 1.7377 mL
40 mM 0.0521 mL 0.2607 mL 0.5213 mL 1.3033 mL
50 mM 0.0417 mL 0.2085 mL 0.4170 mL 1.0426 mL
60 mM 0.0348 mL 0.1738 mL 0.3475 mL 0.8688 mL
80 mM 0.0261 mL 0.1303 mL 0.2607 mL 0.6516 mL
100 mM 0.0209 mL 0.1043 mL 0.2085 mL 0.5213 mL
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AVE-0118 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
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.

Keywords:

AVE-0118498577-53-0AVE0118AVE 0118Potassium ChannelKcsApersistent atrial fibrillationIK,AChItorat small mesenteric artery ring segmentsIKuratrial fibrillationnoradrenalineKv1.5 potassium ion channelalpha-1 adrenergic receptorantiarrhythmic agentInhibitorinhibitorinhibit

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製品名:
AVE-0118
製品番号:
HY-118387
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