Amifampridine phosphate

CAS: 446254-47-3 F: C5H10N3O4P W: 207.12

Amifampridine (3,4-Diaminopyridine) phosphate is an orally active, potent and cell permeable voltage-gated potassium (Kv

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Bioactivity	Amifampridine (3,4-Diaminopyridine) phosphate is an orally active, potent and cell permeable voltage-gated potassium (Kv) channel blocker (PCB). Amifampridine phosphate is efficacy in the reversal of BoNT/A (HY-P79153) intoxication. Amifampridine phosphate increases transmitter release from neuromuscular junctions (NMJs). Amifampridine phosphate can be used for Lambert-Eaton myasthenic syndrome (LEMS) research[1][2][3].
Invitro	Amifampridine phosphate (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 phosphate (0-100 μM) increases the duration of the presynaptic AP (action potential) waveform at mammalian and frog NMJs in a dose-dependent manner[3].
In Vivo	Amifampridine phosphate (Oral gavage; 10 mg/kg; once) can antagonize muscle paralysis following BoNT/A intoxication[2].Amifampridine phosphate (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 phosphate has a short plasma half-life and can induce seizures when present at high concentrations, following penetration of the blood-brain barrier[2]. Animal Model:
Name	Amifampridine phosphate
CAS	446254-47-3
Formula	C5H10N3O4P
Molar Mass	207.12
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[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.

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