Manogepix E1210; APX001A|cas:936339-60-5|西域试剂

Manogepix E1210; APX001A,99.85%

产品编号：Bellancom-18233| CAS NO：936339-60-5| 分子式：C₂₁H₁₈N₄O₂| 分子量：358.39

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货号	价格	库存与货期
Bellancom-18233	￥1650.00	杭州北京（现货）
Bellancom-18233	￥3000.00	杭州北京（现货）
Bellancom-18233	￥13200.00	杭州北京（现货）
Bellancom-18233	￥0.00	杭州北京（现货）

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Manogepix E1210; APX001A

产品介绍

Manogepix (E1210) 是首创的，广谱和口服活性抗真菌药。Manogepix 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

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

体外研究

Manogepix 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 Manogepix is studied and shown to be significantly lower than that on untreated cells. Manogepix inhibits germ tube formation, adherence to polystyrene surfaces, and biofilm formation of C. albicans at concentrations above its MIC.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

Manogepix (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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Specific-pathogen-free female ICR mice (5 weeks; ~25 g) with C. albicans
Dosage:	2.5 mg/kg, 5 mg/kg and 10 mg/kg
Administration:	Oral administration; twice daily; for 3 days
Result:	Reduced the number of viable C. albicans cells in the oral cavity in a dose-dependent manner.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Specific-pathogen-free female ICR mice (5 weeks; ~25 g) with C. albicans
Dosage:	2.5 mg/kg, 5 mg/kg and 10 mg/kg
Administration:	Oral administration; twice daily; for 3 days
Result:	Reduced the number of viable C. albicans cells in the oral cavity in a dose-dependent manner.

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (279.03 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.7903 mL	13.9513 mL	27.9026 mL
5 mM	0.5581 mL	2.7903 mL	5.5805 mL
10 mM	0.2790 mL	1.3951 mL	2.7903 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (5.80 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.80 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (5.80 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.80 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (5.80 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.80 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。