Size | Price | Stock | Qty |
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250mg |
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500mg |
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1g |
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2g |
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Other Sizes |
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Purity: ≥98%
Amifampridinephosphate (trade name: Firdapse; pyridine-3,4-diamine, 3,4-diaminopyridine, 3,4-DAP) is the phosphate salt of Amifampridine, which is an FDA approved drug used mainly in the treatment of a number of rare muscle diseases such as Lambert-Eaton myasthenic syndrome (LEMS) in adults (It 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 |
In HEK293T cells, amifampridine phosphate (1.5 μM) dramatically lowers Kv3.3 and Kv3.4 currents by approximately 10% while having no effect on Cav2.1 or Cav1.2 currents [3]. Amifampridine phosphate (0-100 μM) in humans and frogs lengthens presynaptic AP (action potential) waveforms at the NMJ in a dose-dependent manner [3].
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ln Vivo |
Following BoNT/A poisoning, amifenpyridine phosphate (10 mg/kg; oral gavage; once) can prevent muscular paralysis [2]. Mice's plasma half-life is one hour, while amifenpyridine phosphate (2.5 mg/kg IV; 10 mg/kg PO; once) has a bioavailability (F) of roughly 57% [2]. Amifenpyridine phosphate has a brief plasma half-life and, once past 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 |
C5H10N3O4P
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Molecular Weight |
207.13
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CAS # |
446254-47-3
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Related CAS # |
Amifampridine;54-96-6
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SMILES |
NC1=C(N)C=NC=C1.O=P(O)(O)O
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Chemical Name |
3,4-Diaminopyridine
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Synonyms |
3,6-DAP phosphate; 3,4-Diaminopyridine phosphate; BRN-0110232 phosphate; BRN 0110232; BRN0110232; NSC 521760; NSC-521760; NSC521760 phosphate; 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) |
DMSO:≥ 100 mg/mL
Water:N/A
Ethanol:N/A
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Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 4.8279 mL | 24.1394 mL | 48.2789 mL | |
5 mM | 0.9656 mL | 4.8279 mL | 9.6558 mL | |
10 mM | 0.4828 mL | 2.4139 mL | 4.8279 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.