1. PI3K/Akt/mTOR Anti-infection
  2. Akt HIV Parasite
  3. Miltefosine

Miltefosine  (Synonyms: 米替福新; HePC; Hexadecyl phosphocholine)

目录号: HY-13685 纯度: ≥98.0%
COA 产品使用指南

Miltefosine是一种广谱抗微生物,抗利什曼原虫,磷脂剂,通过抑制 PI3K/Akt 活性起作用。Miltefosine 是 CTP 磷酸胆碱胞苷基转移酶 (CCT) 的抑制剂

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Miltefosine Chemical Structure

Miltefosine Chemical Structure

CAS No. : 58066-85-6

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3.  试用装只面向终端客户

规格 价格 是否有货 数量
10 mM * 1 mL in Water ¥660
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100 mg ¥600
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500 mg ¥1400
In-stock
1 g ¥1874
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Top Publications Citing Use of Products
  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

Miltefosine is a broad spectrum antimicrobial, anti-leishmanial, phospholipid agent acting by inhibiting the PI3K/Akt activity[1][2][3][4]. Miltefosine is an inhibitor of CTP-phosphocholine cytidyltransferase (CCT)[5].

IC50 & Target[1]

HIV-1

 

体外研究
(In Vitro)

用 Miltefosine 处理 HIV-1 感染的巨噬细胞会抑制 PH-AktGFP 向质膜的募集。由于 Miltefosine 通过模拟 PH 结构域抑制 Akt,因此 Miltefosine 很可能与 PIP3 结合,从而阻止 PH-Akt 向膜募集[1]。Miltefosine (HePC) 在无细胞提取物中抑制来自 NIH3T3 细胞的蛋白激酶 C (PKC),IC50 约为 7 μM。抑制与磷脂酰丝氨酸具有竞争性,Ki 为 0.59 μM[2]。Miltefosine 是一种烷基磷脂,可抑制 Akt 的激活。Miltefosine 是 Akt 的直接抑制剂,在培养物中诱导原发性渗出性淋巴瘤 (PEL) 的剂量依赖性抑制,还抑制 Akt 的下游靶标,例如 mTOR,从而导致 S6K 和 S6 的磷酸化和活化减少。重要的是,Miltefosine 还抑制不属于 mTOR 通路一部分的 Akt 靶标,例如 FOXO1,因此预计其处理效果比单独使用 mTORC1 抑制剂更大[3]

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

体内研究
(In Vivo)

将小鼠随机分为 5 组,每周 5 天腹膜内注射 50 mg/kg 溶解在 PBS 中的 Miltefosine 或哌立福新,或等效体积的载体 (PBS)。与媒介物处理的小鼠相比,Miltefosine 和 Perifosine 均能抑制肿瘤的生长速度。到处理后第 14 天,与媒介物处理的小鼠相比,派立福新和 Miltefosine 处理的小鼠的平均肿瘤体积减少了约 50% (P<0.04)。肿瘤生长也显著延迟 (通过线性混合效应模型分析,Perifosine P < 0.04 和 Miltefosine P ≤ 0.055)。免疫组织化学分析显示,与 PBS 处理的小鼠相比,Miltefosine 和哌立福新处理的小鼠肿瘤切片中磷酸化核糖体 S6 蛋白的染色总体减少。这种减少的磷酸化与药物处理动物的肿瘤进展延迟相关[3]

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

Clinical Trial
分子量

407.57

Formula

C21H46NO4P

CAS 号
性状

固体

颜色

White to off-white

中文名称

米替福新

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
In solvent -80°C 2 years
-20°C 1 year
溶解性数据
In Vitro: 

H2O 中的溶解度 : 33.33 mg/mL (81.78 mM; 超声助溶 (<60°C))

DMSO 中的溶解度 : 3.33 mg/mL (8.17 mM; 超声助溶 (<60°C); 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.4536 mL 12.2678 mL 24.5357 mL
5 mM 0.4907 mL 2.4536 mL 4.9071 mL
查看完整储备液配制表

* 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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

* 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

In Vivo:

以下溶解方案,请直接配置工作液。建议现用现配,在短期内尽快用完。 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。

  • 方案 一

    请依序添加每种溶剂: PBS

    Solubility: 100 mg/mL (245.36 mM); 澄清溶液; 超声助溶

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
该产品水溶性佳,请具体参考实测 水 / PBS / Saline 中的溶解度数据。
您所需的储备液浓度超过该产品的实测溶解度,如有需要,请与 MCE 中国技术支持联系。
纯度 & 产品资料

纯度: ≥98.0%

参考文献
Kinase Assay
[3]

Levels of enzymatically active caspase-3 are quantified using the ApoAlert Caspase Fluorescent assay kit. Briefly, 1×106 BC-1 PEL cells are treated with 50 μM Miltefosine, 50 μM Perifosine, or 20 nM NVP-BEZ235, as well as the respective vehicle controls. Cells are harvested and lysed 12 hours later. Equivalent micrograms of cell lysate for all samples are incubated with a fluorogenic caspase-3 substrate (DEVD-AFC). Cleavage of DEVD by caspase-3 releases AFC, the fluorescence of which is measured using a FLUOstar OPTIMA fluorometer, with excitation and emission filter wavelengths set to 400 and 505 nm, respectively[3].

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

Cell Assay
[2]

NIH3T3 cells are grown in DMEM supplemented with 10% FCS in a humidified atmosphere of 95% air with 5% CO2. Cells are plated on 35-mm culture dishes (6-well plates) at 0.5-0.8×105 cells/well. Growth is established for 18-24 h and the cell number of representative wells is determined (time 0). The experiments are started by addition of fresh prepared solution of Miltefosine at given concentrations to the cells or equal volumes of Tris-HCI to control cells. After incubation for 60 h, cells are counted with an electronic counter. Cellular multiplication is calculated[2].

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

Animal Administration
[3][4]

Mice[3]
PEL cells are washed in ice-cold phosphate buffered saline, counted, and diluted in 100 μL of PBS mixed with 100 μL of growth factor-depleted Matrigel. A total of 1×105 to 7.5×105 BC-1 cells are injected subcutaneously into the right flank of NOD.CB17-Prkdcscid/J or CB17-Prkdcscid/J mice. The mice are monitored on alternate days for development of palpable tumors (2 mm3), at which point drug or vehicle treatments are initiated, and are administered either intraperitoneally (Perifosine) or by oral gavage (Rosiglitazone, NVP-BEZ235) 5 days a week. Groups of 5 to 7 mice are used to generate PEL tumors and treated with either vehicle or drug cocktail. Each biologic experiment is repeated multiple times. For Rosiglitazone, 0.25% methylcellulose is used as vehicle, and 30 mg/kg or 60 mg/kg Rosiglitazone is suspended in methylcellulose. For Perifosine and Miltefosine, PBS is used as a vehicle and 50 mg/kg Perifosine or Miltefosine is dissolved in PBS. For NVP-BEZ235, the compound is dissolved in a 1:9 vol/vol mixture of 1-methyl-2-pyrrolidone and polyethylene glycol 300. A dose of 40 mg/kg NVP-BEZ235 or equal volume of the vehicle is administered. Tumor diameters are measured using digital calipers, and tumor volume is calculated. The tumors are excised and fixed in formalin. Statistical analyses are performed using linear model fit by maximum likelihood with individual animals treated as random effect.
Rats[4]
Male Sprague-Dawley rats (weight 270-290 g) are divided into five groups (n=5). Rats in the treatment groups are administered a single 10 mg/kg oral dose of Miltefosine (MFS) either as an aqueous solution or MFS-LNCs dispersion by gastric gavage. This dose is equivalent to the 20 mg/kg Miltefosine dose administered to mice in the preclinical study after correction for rats. Following administration, blood samples are collected via the orbital plexus under anesthesia at time intervals of 0.5, 1, 2, 4, 7, 10, 24, 48, 72 and 216 h in Eppendorf tubes containing EDTA. Blood samples are then centrifuged immediately at 4000 rpm for 10 min. Plasma samples are frozen and maintained at -80°C pending analysis.

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

参考文献

Miltefosine 相关分类

完整储备液配制表

* 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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO / H2O 1 mM 2.4536 mL 12.2678 mL 24.5357 mL 61.3392 mL
5 mM 0.4907 mL 2.4536 mL 4.9071 mL 12.2678 mL
H2O 10 mM 0.2454 mL 1.2268 mL 2.4536 mL 6.1339 mL
15 mM 0.1636 mL 0.8179 mL 1.6357 mL 4.0893 mL
20 mM 0.1227 mL 0.6134 mL 1.2268 mL 3.0670 mL
25 mM 0.0981 mL 0.4907 mL 0.9814 mL 2.4536 mL
30 mM 0.0818 mL 0.4089 mL 0.8179 mL 2.0446 mL
40 mM 0.0613 mL 0.3067 mL 0.6134 mL 1.5335 mL
50 mM 0.0491 mL 0.2454 mL 0.4907 mL 1.2268 mL
60 mM 0.0409 mL 0.2045 mL 0.4089 mL 1.0223 mL
80 mM 0.0307 mL 0.1533 mL 0.3067 mL 0.7667 mL

* 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

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