Amifampridine
Based on 1 Customer Validation
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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- Purity: 99.99%
- CAS No.: 54-96-6
- 화학식: C5H7N3
- 분자량:109.13
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보관:
Store at room temperature 3 years.
In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Biological Activity
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 (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.
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Animal Model:CD-1 mouse (female,25 g, 6 weeks old)[2]
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Dosage:10 mg/kg
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Administration:Oral gavage, once, after BoNT/A administration (IP)
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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.
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Animal Model:CD-1 mouse (30-35 g, 8 weeks old)[2]
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Dosage:2.5 mg/kg (IV); 10 mg/kg (PO)
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Administration:IV, orally, once (Pharmacokinetic Analysis)
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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
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 54-96-6
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Appearance Solid
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분자량 109.13
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화학식 C5H7N3
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Color Off-white to gray
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SMILES
NC1=C(N)C=CN=C1
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Synonyms
3,4-Diaminopyridine
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Store at room temperature 3 years
In solvent -80°C 2 years -20°C 1 year
용액&용해도
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)
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
순도&문서
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Data Sheet (280 KB)
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SDS (480 KB)
- English - EN (480 KB)
- Français - FR (480 KB)
- Deutsch - DE (480 KB)
- Norwegian - NO (480 KB)
- Español - ES (480 KB)
- Swedish - SV (480 KB)
- Italian - IT (480 KB)
- Korean - KR (480 KB)
- Portuguese - PT (480 KB)
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Handling Instructions (2659 KB)
References
[1]. Maarten J Titulaer, et al. Lambert-Eaton myasthenic syndrome: from clinical characteristics to therapeutic strategies. Lancet Neurol. 2011 Dec;10(12):1098-107. [Content Brief]
[2]. T L Harris, et al. Lycopodium clavatum exine microcapsules enable safe oral delivery of 3,4-diaminopyridine for treatment of botulinum neurotoxin A intoxication. Chem Commun (Camb). 2016 Mar 18;52(22):4187-90. [Content Brief]
[3]. Ojala KS, et al. A high-affinity, partial antagonist effect of 3,4-diaminopyridine mediates action potential broadening and enhancement of transmitter release at NMJs. J Biol Chem. 2021 Jan-Jun;296:100302. [Content Brief]
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| 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 |
Amifampridine Related Classifications
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