Amifampridine
目录号: PL09965 纯度: ≥99%
CAS No. :54-96-6
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中文名称
Amifampridine
中文别名
3,4-二氨基吡啶;2-氨基烟酸甲酯;3,4-Diaminopyridine 3,4-二氨基吡啶;5-(戊烷-3-基氧基)-7-氧杂双环(4.1.0)庚-3-烯-3-羧酸乙酯;吡啶-3,4-二胺;阿米吡啶
英文名称
Amifampridine
英文别名
Pyridine-3,4-diamine;3,4-Diaminopyridine;3.4-Diaminopyridine;3,4 DI AMINO PYRIDINE;3,4-diamino-pyridin;3,4-Diaminopyridin;3,4-diamino-pyridine;3,4-DIAMINOPYRIDINE FOR SYNTHESIS;3,4-pyridinediamine;3,4-Pyridinedramine;3-amino-4-pyridinylamine;4,5-diaminopyridine;Amifampridine;diamino-3,4pyridine;pyridin-3,4-diaMine;AC-907/34116043;Amifampridine (USAN/INN);STK503647;Pyridine,4-diamino-;D10228;3,4-DAP;NSC790505;Pyridine, 3,4-diamino-;AMIFAMPRIDINE [USAN];NSC-521760;SC10;NSC521760;NSC-790505;A7976;Amifampridine [INN];NCGC00167560-01;PB48915;NSC 521760;W-105592;Z385438794;InChI=1/C5H7N3/c6-4-1-2-8-3-5(4)7/h1-3H,7H2,(H2,6,8;amifampridin;Dynamine;FT-0614203;HMS2233K06;BCP22343;MFCD00006401;Q411707;NCGC00167560-02;SMR000752913;AMIFAMPRIDINE [WHO-DD];DB11640;BRN 0110232;3,4-Diammoniopyridinium;UNII-RU4S6E2G0J;3,4-DIAMINOPYRIDINE;CHEBI:135948;3,4-diamino pyridine;PS-9273;Nc1ccncc1N;AMIFAMPRIDINE [ORANGE BOOK];pyridine-3,4-diamine;Diamino-3,4 pyridine;CCG-304141;3,4 DIAMINOPYRIDINE [VANDF];HY-14946;Ruzurgi;F0001-1409;MLS001333182;LS-131135;AMIFAMPRIDINE [MART.];DTXCID4026715;Amifampridine [USAN:INN:BAN];L89;GTPL8032;Tox21_112555;CAS-54-96-6;CL0116;MLS001333181;D1149;BP-12781;3,4-diaminopyridin;Tox21_112555_1;54-96-6 (free base);Amifampridine [INN:BAN];3,4-Pyridinediamine;AM20070030;5-22-11-00266 (Beilstein Handbook Reference);BDBM50416493;SCHEMBL21273;4-DAP;MLS001304911;EN300-69695;54-96-6;CHEMBL354077;EINECS 200-220-9;WLN: T6NJ CZ DZ;DTXSID6046715;BBL013269;AKOS000672436;AMIFAMPRIDINE [MI];3,4 Diaminopyridine;J-610017;s4622;AMIFAMPRIDINE [EMA EPAR];Ruzurgi (TN);RU4S6E2G0J;4,5-Diaminopyridine
Cas No.
54-96-6
分子式
C5H7N3
分子量
109.13
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
Amifampridine (3,4-Diaminopyridine) 是一种口服有效和可透过细胞的电压门控钾 (Kv) 通道阻断剂 (PCB)。Amifampridine 对 BoNT/A (HY-P79153) 中毒有明显的逆转作用。Amifampridine 可增加神经肌肉连接 (NMJs) 的递质释放。Amifampridine 可用于 Lambert-Eaton 肌无力综合征 (LEMS) 的研究。
生物活性
Amifampridine (3,4-Diaminopyridine) is an orally active, potent and cell permeable voltage-gated potassium (K v ) 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.
性状
Solid
体外研究(In Vitro)
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.
Amifampridine (0-100 μM) increases the duration of the presynaptic AP (action potential) waveform at mammalian and frog NMJs in a dose-dependent manner. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
Amifampridine (Oral gavage; 10 mg/kg; once) can antagonize muscle paralysis following BoNT/A intoxication.
Amifampridine (2.5 mg/kg (IV); 10 mg/kg (PO); once) shows 1 hour plasma half-life and about 57% bioavailability (F) in mice.
Amifampridine has a short plasma half-life and can induce seizures when present at high concentrations, following penetration of the blood-brain barrier. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
ClinicalTrial
参考文献
[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.
溶解度数据
In Vitro: DMSO : ≥ 38 mg/mL (348.21 mM)配制储备液
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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