010-60605840
结构式搜索
  1. 首页
  2. 产品目录
  3. Signaling Pathways(信号通路)
  4. PI3K/Akt/mTOR
  5. AKT
中文名称: 米替福新 促销 热销  一键复制产品信息
英文名称: Miltefosine
CAS No: 58066-85-6
分子式: C21H46NO4P
分子量: 407.57
安全技术说明书 MSDS 产品说明书 技术规格说明书 产品使用指南
M60007 米替福新 ≥98% (普西唐-psaitong)
熔点：
232.2-233.9°C
包装规格：
500mg 1g 5g in glass bottle
溶解性：
溶于水(10mg/ml)、DMSO(800μg/ml)、乙醇(1mg/ml)
产品描述：

基本信息

产品编号：

M60007

产品名称：

Miltefosine

CAS:

58066-85-6

 

储存条件

粉末

-20℃

四年

 

 

分子式：

C21H46NO4P

溶于液体

-80℃

6个月

分子量：

407.57

-20℃

1个月

化学名： 

HePC Hexadecyl phosphocholine

Solubility (25°C)：

 

体外:

 

DMSO

Insoluble

Ethanol

81mg/mL (198.73mM)

Water

81mg/mL (198.73mM)

体内(现配现用):

Saline

30mg/mL

＜1mg/ml表示微溶或不溶。

普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。

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。

 

制备储备液

 

浓度

 

溶液体积

质量

 

1mg

 

5mg

 

10mg

1mM

2.4536mL

12.2678mL

24.5357mL

5mM

0.4907mL

2.4536mL

4.9071mL

10mM

0.2454mL

1.2268mL

2.4536mL

 

生物活性

产品描述

一种诱导组胺释放的PI-3/Akt抑制剂，ED50分别为17.2μM和8.1μM。

靶点

Akt;HIV-1

体外研究

Treatment of HIV-1 infected macrophages with Miltefosine inhibits the recruitment of PH-AktGFP to the plasma membrane.Since Miltefosine inhibits Akt through mimicry of the PH domain,it is likely that Miltefosine binds to PIP3,blocking the recruitment of PH-Akt to the membrane.Miltefosine (HePC) inhibits protein kinase C (PKC) from NIH3T3 cells in cell-free extracts with a IC50 of about 7µM.Inhibition is competitive with regard to phosphatidylserine with a Ki of 0.59µM.Miltefosine is an alkylphospholipid that inhibit activation of Akt.Miltefosine is a direct inhibitor of Akt,and induces dosedependent inhibition of primary effusion lymphoma (PEL) in culture and also inhibits the downstream targets of Akt,such as mTOR,leading to reduced phosphorylation and activation of S6K and S6.Importantly,Miltefosine also inhibits Akt targets that are not part of the mTOR pathway,eg,FOXO1,and are therefore expected to have a greater therapeutic impact than mTORC1 inhibitors alone.

体内研究

Mice are randomized into groups of 5 and injected intraperitoneally 5 days a week with 50mg/kg of either Miltefosine or Perifosine dissolved in PBS,or equivalent volume of vehicle (PBS).Both Miltefosine and Perifosine inhibit the growth rate of tumors compared with vehicle-treated mice.By day 14 after treatment,there is an approximately 50% decrease in average tumor volume in Perifosine-and Miltefosine-treated mice,compared with vehicle-treated mice (P<0.04).Tumor growth is also significantly retarded (P<0.04 for Perifosine and P≤0.055 for Miltefosine by linear mixed-effects model analysis).Immunohistochemical analyses display an overall reduction in staining for phosphorylated ribosomal S6 protein in tumor sections from Miltefosine- and Perifosine-treated mice compared with the PBS-treated mice.This reduced phosphorylation correlated with the delay in tumor progression in drug-treated animals.

 

推荐实验方法(仅供参考)

激酶实验：

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 50μM Miltefosine,50μM Perifosine,or 20nM 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 505nm,respectively.

 

细胞实验:

 

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 18-24h 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 60h,cells are counted with an electronic counter.Cellular multiplication is calculated.

 

动物实验:

 

Mice

PEL cells are washed in ice-cold phosphate buffered saline, counted,and diluted in 100μL of PBS mixed with 100μL 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 30mg/kg or 60mg/kg Rosiglitazone is suspended in methylcellulose.For Perifosine and Miltefosine,PBS is used as a vehicle and 50mg/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 40mg/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

Male Sprague-Dawley rats (weight 270-290g) are divided into five groups (n=5).Rats in the treatment groups are administered a single 10mg/kg oral dose of Miltefosine (MFS) either as an aqueous solution or MFS-LNCs dispersion by gastric gavage.This dose is equivalent to the 20mg/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 216h 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℃ pending analysis.
保存条件：
-20℃
UN码：
HazardClass：
危害声明：
安全说明：
搜索质检报告(COA)

分析证书(COA)

Lot/Batch Number

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)

摩尔浓度计算公式

  • =
    *
    *
    *选择对应的单位 *空出希望得到的变量，填写另外两个变量

用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为：C1V1 = C2V2 ( 输入 输出 )

  • * = *

连续稀释计算器方程

  • 连续稀释

  • 初始浓度:
  • 稀释倍数:

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
​
请在下列方框中输入相关信息后点击计算，可以得到母液配置方法和体内配方的制备方法：
举例：给药剂量是10 mg/kg，每只动物体重20g，给药体积100 μL， TargetMol | Animal experiments  一共给药动物10只，您使用的配方为5%TargetMol | reagent DMSO + 30%PEG300 + 5%Tween 80 + 60%Saline/PBS/ddH2O， 那么您的工作液浓度为2mg/mL。
母液配置方法: 2 mg 药物溶于 50 μLDMSOTargetMol | reagent  （ 母液浓度为 40 mg/mL ）, 如您需要配置的浓度超过该产品的溶解度，请先与我们客服联系。
体内配方的制备方法: 取 50μLDMSOTargetMol | reagent  母液，添加 300 μLPEG300TargetMol | reagent  混匀澄清，再加 50μLTween80, 混匀澄清，再加 600μLSaline/PBS/ddH2OTargetMol | reagent ​ 混匀澄清

方案所需的各种助溶剂如： DMSO ， PEG300 / PEG400 ， Tween 80 ， SBE-β-CD ， 玉米油 等， 均可点击跳转或在网站搜索购买。
 
以上为“动物实验计算换算器”的使用方法举例，并不是具体某个试剂的配制，请根据您的实验动物和给药方式选择适当的溶解方案。
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系普西唐客服为您提供正确的澄清溶液配方）
+
+
+
计算 重置

计算结果:

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，

体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL Saline/PBS/ddH2O，混匀澄清。

1. 首先保证母液是澄清的；
           2. 一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

剂量转换

对于不同动物的给药剂量换算，您也可以参考 更多
购物指南
参考资料
支付方式
关于配送
售后服务
微信二维码
首页 |网站使用条款 |隐私政策 |关于我们 |营业执照 |结构式搜索
© 2001-2020 北京普西唐生物科技有限公司  天津普西唐生物医药科技有限公司
版权所有，并保留所有权利 
备案号：京ICP备17064988号-1