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E1210

(Synonyms: E1210; APX001A)

目录号: PL14622 纯度: ≥99%

E1210 (APX001A) 是首创的，广谱和口服活性抗真菌药。E1210 具有抑制真菌糖基磷脂酰肌醇生物合成的作用机制。

CAS No. :936339-60-5

商品编号	规格	价格	会员价
PL14622-5mg	5mg	¥1175.00	请登录
PL14622-10mg	10mg	¥1925.00	请登录
PL14622-50mg	50mg	¥4775.00	请登录
PL14622-100mg	100mg	¥6815.00	请登录
PL14622-10mM*1mLinDMSO	10mM*1mLinDMSO	¥2925.00	请登录
PL14622-1 mL x 10 mM (in DMSO)		¥942.00	请登录

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中文名称	E1210
英文名称	E1210
英文别名	E1210;7B1P18ID9L;E 1210;WSEKTEUGRLFBSE-UHFFFAOYSA-N;Q15410951;3-[3-[[4-(2-pyridyloxymethyl)phenyl]methyl]isoxazol-5-yl]pyridin-2-amine;3-[3-[4-(2-Pyridyloxymethyl)benzyl]isoxazole-5-yl]pyridine-2-amine;3-(3-(4-((Pyridin-2-yloxy)methyl)benzyl)isoxazol-5-yl)pyridin-2-amine;3-(3-(4(Pyridin-2-yloxymethyl)-benzyl)-isoxazol-5yl)-pyridin-2-ylamine;3-(3-(4-(Pyridin-2-yloxymethyl)-benzyl)-isoxazol-5-yl)-pyridin-2-ylam;3-[3-[[4-(Pyridin-2-yloxymethyl)phenyl]methyl]-1,2-oxazol-5-yl]pyridin-2-amine;Manogepix;3-[3-[[4-[(2-Pyridinyloxy)methyl]phenyl]methyl]-5-isoxazolyl]-2-pyridinamine (ACI);3-[3-[4-[(Pyridin-2-yloxy)methyl]benzyl]isoxazol-5-yl]pyridin-2-amine;[3-[3-[4-[[(Pyridin-2-yl)oxy]methyl]benzyl]isoxazol-5-yl]pyridin-2-yl]amine;APX 001A;E 1210 (pharmaceutical)
Cas No.	936339-60-5
分子式	C₂₁H₁₈N₄O₂
分子量	358.39
包装储存	Powder -20°C 3 years；4°C 2 years
详情描述	E1210 (APX001A) 是首创的，广谱和口服活性抗真菌药。E1210 具有抑制真菌糖基磷脂酰肌醇生物合成的作用机制。

产品详情

E1210 (APX001A) 是首创的，广谱和口服活性抗真菌药。E1210 具有抑制真菌糖基磷脂酰肌醇生物合成的作用机制。

生物活性

E1210 (APX001A) is a first-in-class, broad-spectrum and orally active antifungal. E1210 has a mechanism of action-inhibition of fungal glycosylphosphatidylinositol (GPI) biosynthesis.

性状

Solid

IC50 & Target[1][2]

Fungal

体外研究(In Vitro)

E1210 inhibits the inositol acylation activity of C. albicans Gwt1p and A. fumigatus Gwt1p with IC50s of 0.3 to 0.6 μM but has no inhibitory activity against human Pig-Wp even at concentrations as high as 100 μM. To confirm the inhibition of fungal glycosylphosphatidylinositol (GPI) biosynthesis, expression of ALS1 protein, a GPI-anchored protein, on the surfaces of C. albicans cells treated with E1210 is studied and shown to be significantly lower than that on untreated cells. E1210 inhibits germ tube formation, adherence to polystyrene surfaces, and biofilm formation of C. albicans at concentrations above its MIC. has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

E1210 (2.5 mg/kg, 5 mg/kg and 10 mg/kg; oral administration; twice daily; for 3 days; specific-pathogen-free female ICR mice) treatment reduces the number of viable C. albicans cells in the oral cavity in a dose-dependent manner. 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]. Watanabe NA, et al. E1210, a new broad-spectrum antifungal, suppresses Candida albicans hyphal growth through inhibition of glycosylphosphatidylinositol biosynthesis. Antimicrob Agents Chemother. 2012 Feb;56(2):960-71.
[2]. Hata K, et al. Efficacy of oral E1210, a new broad-spectrum antifungal with a novel mechanism of action, in murine models of candidiasis, aspergillosis, and fusariosis. Antimicrob Agents Chemother. 2011 Oct;55(10):4543-51.

溶解度数据	In Vitro: DMSO : 100 mg/mL (279.03 mM; Need ultrasonic)配制储备液

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产品使用指南

Data Sheet

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。

E1210

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