Size | Price | Stock | Qty |
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50mg |
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100mg |
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250mg |
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500mg |
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1g |
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2g |
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5g |
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Other Sizes |
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Purity: ≥98%
Amifampridine (trade name: Firdapse; pyridine-3,4-diamine, 3,4-diaminopyridine, 3,4-DAP) is an FDA approved drug used predominantly in the treatment of a number of rare muscle diseases such as Lambert-Eaton myasthenic syndrome (LEMS) in adults. It was developed by Catalyst pharmaceuticals and gained US approval in November 2018). The free base form of the drug has been used to treat congenital myasthenic syndromes and Lambert–Eaton myasthenic syndrome (LEMS) through compassionate use programs since the 1990s and was recommended as a first line treatment for LEMS in 2006, using ad hoc forms of the drug, since there was no marketed form.
ln Vitro |
Cav2.1 and Cav1.2 currents in HEK293T cells are unaffected by amifampridine (1.5 μM), whereas Kv3.3 and Kv3.4 currents are severely reduced by about 10% [3]. In frogs and humans, amifampridine (0-100 μM) dose-dependently lengthens the presynaptic AP (action potential) waveforms at the NMJ [3].
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ln Vivo |
After being intoxicated with BONT/A, amifampridine (10 mg/kg; once) can counteract muscular paralysis [2]. Amifampridine has an hour-long plasma half-life and a roughly 57% bioavailability (F) in mice when administered once at doses of 2.5 mg/kg (IV) and 10 mg/kg (PO) [2]. Amifampridine has a relatively short plasma half-life and, after crossing the blood-brain barrier, can cause epileptic seizures at high concentrations [2].
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Animal Protocol |
Animal/Disease Models: CD-1 mice (female, 25 g, 6 weeks old) [2]
Doses: 10 mg/kg Route of Administration: BoNT/A administration (IP) followed by po (oral gavage) once (IP) Experimental Results: demonstrated that either LEM alone (182 ± 43 minutes) or the maximum safe oral dose of 3,4-DAP alone (225 ± 24 minutes) Dramatically increased the time to death after toxin administration (216 ± 29 minutes). 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 minutes, a 40% increase compared to toxin alone. Animal/Disease Models: CD-1 mice (30-35 g, 8 weeks old) [2] Doses: 2.5 mg/kg (IV); 10 mg/kg (PO) Route of Administration: intravenous (iv) (iv)injection, oral administration, once (drug pharmacokinetic/PK/PK analysis) Experimental Results: pharmacokinetic/PK/PK parameters of Amifampridine in CD-1 mice [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 |
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.
[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. [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. |
Molecular Formula |
C5H7N3
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Molecular Weight |
109.13
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CAS # |
54-96-6
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Related CAS # |
Amifampridine phosphate;446254-47-3
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SMILES |
NC1=C(N)C=NC=C1
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Chemical Name |
3,4-Diaminopyridine
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Synonyms |
3,6-DAP; 3,4-Diaminopyridine; BRN-0110232; BRN 0110232; BRN0110232; NSC 521760; NSC-521760; NSC521760; SC10; Trade name: Firdapse.
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (22.91 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (22.91 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (22.91 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.