2. Membrane Transporter/Ion Channel
  3. Potassium Channel
  4. Amifampridine

Amifampridine  (Synonyms: 3,4-ジアミノピリジン; 3,4-Diaminopyridine)

製品番号: HY-14946 純度: 99.99%
COA 取扱説明書 Technical Support

Amifampridine (3,4-Diaminopyridine) is an orally active, potent and cell permeable voltage-gated potassium (Kv) channel blocker (PCB). Amifampridine is efficacy in the reversal of BoNT/A (HY-P79153) intoxication. Amifampridine increases transmitter release from neuromuscular junctions (NMJs). Amifampridine can be used for Lambert-Eaton myasthenic syndrome (LEMS) research.

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Amifampridine

Amifampridine 構造式

CAS 番号 : 54-96-6

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 27 在庫あり
Solution
10 mM * 1 mL in DMSO USD 27 在庫あり
Solid
10 g $25 在庫あり
25 g $52 在庫あり
50 g $90 在庫あり
100 g $154 在庫あり
> 100 g   お問い合わせ  

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Amifampridine 関連抗体

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製品説明

Amifampridine (3,4-Diaminopyridine) is an orally active, potent and cell permeable voltage-gated potassium (Kv) channel blocker (PCB). Amifampridine is efficacy in the reversal of BoNT/A (HY-P79153) intoxication. Amifampridine increases transmitter release from neuromuscular junctions (NMJs). Amifampridine can be used for Lambert-Eaton myasthenic syndrome (LEMS) research[1][2][3].

体外実験

Amifampridine (1.5 μM) significantly reduces Kv3.3 and Kv3.4 currents by about 10% in HEK293T cells, has no effect on Cav2.1 or Cav1.2 current[3].
Amifampridine (0-100 μM) increases the duration of the presynaptic AP (action potential) waveform at mammalian and frog NMJs in a dose-dependent manner[3].

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

Amifampridine 関連抗体
体内実験

Amifampridine (Oral gavage; 10 mg/kg; once) can antagonize muscle paralysis following BoNT/A intoxication[2].
Amifampridine (2.5 mg/kg (IV); 10 mg/kg (PO); once) shows 1 hour plasma half-life and about 57% bioavailability (F) in mice[2].
Amifampridine has a short plasma half-life and can induce seizures when present at high concentrations, following penetration of the blood-brain barrier[2].

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

Animal Model: CD-1 mouse (female,25 g, 6 weeks old)[2]
Dosage: 10 mg/kg
Administration: Oral gavage, once, after BoNT/A administration (IP)
Result: Revealed that neither LEMs alone (182 ± 43 min) nor the maximum safe orally deliverable dose of 3,4-DAP alone (225 ± 24 min) could significantly increase the time to death following toxin administration (216 ± 29 min). However, when the 10/50/40 3,4-DAP/LEM/shellac formulation was administered at 25 mg/kg the time to death was 302 ± 26 min - a 40% increase as compared to toxin alone.
Animal Model: CD-1 mouse (30-35 g, 8 weeks old)[2]
Dosage: 2.5 mg/kg (IV); 10 mg/kg (PO)
Administration: IV, orally, once (Pharmacokinetic Analysis)
Result: Pharmacokinetic Parameters of Amifampridine in CD-1 mouse[1].
IV (2.5 mg/kg) PO (10 mg/kg)
t1/2 (h) 1.04 1.28
AUC0-24 (μM·h) 4.29 9.72
F (%) 100 56.7
臨床実験
分子量

109.13

分子式

C5H7N3
CAS 番号
Appearance

Solid

Color

Off-white to gray

SMILES

NC1=C(N)C=CN=C1
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

Store at room temperature 3 years

*In solvent : -80°C, 6 months; -20°C, 1 month (Store at room temperature 3 years)
溶剤 & 溶解度
体外: 

DMSO : 100 mg/mL (916.34 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 9.1634 mL 45.8169 mL 91.6338 mL
5 mM 1.8327 mL 9.1634 mL 18.3268 mL
10 mM 0.9163 mL 4.5817 mL 9.1634 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

  • 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
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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

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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 (22.91 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 (22.91 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

純度: 99.99%

COA (250 KB) HNMR (116 KB) RP-HPLC (218 KB)

取扱説明書 (2659 KB)
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 9.1634 mL 45.8169 mL 91.6338 mL 229.0846 mL
5 mM 1.8327 mL 9.1634 mL 18.3268 mL 45.8169 mL
10 mM 0.9163 mL 4.5817 mL 9.1634 mL 22.9085 mL
15 mM 0.6109 mL 3.0545 mL 6.1089 mL 15.2723 mL
20 mM 0.4582 mL 2.2908 mL 4.5817 mL 11.4542 mL
25 mM 0.3665 mL 1.8327 mL 3.6654 mL 9.1634 mL
30 mM 0.3054 mL 1.5272 mL 3.0545 mL 7.6362 mL
40 mM 0.2291 mL 1.1454 mL 2.2908 mL 5.7271 mL
50 mM 0.1833 mL 0.9163 mL 1.8327 mL 4.5817 mL
60 mM 0.1527 mL 0.7636 mL 1.5272 mL 3.8181 mL
80 mM 0.1145 mL 0.5727 mL 1.1454 mL 2.8636 mL
100 mM 0.0916 mL 0.4582 mL 0.9163 mL 2.2908 mL
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Amifampridine 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:

Amifampridine54-96-63,4-DiaminopyridinePotassium ChannelKcsAneuromuscular junctionvoltage-gated potassiumKvneurological diseaseLEMSmyasthenic syndromeOralInhibitorinhibitorinhibit

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