中文名称: AP20187
英文名称: AP20187
CAS No: 195514-80-8
分子式: C82H107N5O20
分子量: 1482.75
A11601 AP20187 ≥98% (psaitong)
包装规格:
1mg in glass bottle
溶解性:
溶于DMSO(≥57mg/mL)
产品描述:

基本信息

产品编号:A11601

产品名称:AP20187

CAS:

195514-80-8

 

储存条件

粉末

-20℃

四年

 

 

分子式:

C82H107N5O20

溶于液体

-80℃

六个月

分子量

1482.75

-20℃

一个月

化学名: 

[(1R)-3-(3,4-dimethoxyphenyl)-1-[3-[2-[[2-[[[2-[3-[(1R)-3-(3,4-dimethoxyphenyl)-1-[(2S)-1-[(2S)-2-(3,4,5-trimethoxyphenyl)butanoyl]piperidine-2-carbonyl]oxypropyl]phenoxy]acetyl]amino]methyl]-3-(dimethylamino)propyl]amino]-2-oxoethoxy]phenyl]propyl] (2S)-1-[(2S)-2-(3,4,5-trimethoxyphenyl)butanoyl]piperidine-2-carboxylate

 

Solubility (25°C)

 

体外

DMSO

≥57mg/mL (38.44mM)

Ethanol

100mg/mL (67.44mM; Need ultrasonic)

Water

 

体内

现配现用

 

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

0.6744mL

3.3721mL

6.7442mL

5mM

0.1349mL

0.6744mL

1.3488mL

10mM

0.0674mL

0.3372mL

0.6744mL

 

 

生物活性

产品描述

一种细胞渗透性分子,使 FK506 结合蛋白 (FKBP) 二聚化,启动生物信号传导级联反应和基因表达,或破坏蛋白-蛋白之间相互作用。

靶点/IC50

FKBP homodimerizer

 

体外研究

When LNCaP cells are treated with AP20187 (B/B Homodimerizer) (100nM), ro-iCaspase-9 levels are significantly reduced,and the smaller processed active caspase-9 becomes apparent.

 

体内研究

Real-time PCR analysis shows that AP20187 (B/B Homodimerizer) (0.5 mg/kg, 2 mg/kg, or 5mg/kg) treatment significantly increases the levels of CHOP mRNA in the CNS of PLP/Fv2E-PERK mice at PID12. AP20187 treatment significantly alleviates EAE-induced myelin damage in these mice. AP20187 (B/B Homodimerizer) treatment significantly reduces the number of degenerating axons and increases the density of axons in the demyelinating lesions in the lumbar spinal cord of PLP/Fv2EPERK mice

 

 

 

推荐实验方法(仅供参考)

细胞实验:

Cell Assay

For the in vitro study, 16 h after ADV infection, cells are treated with R1881 (10nM), AP20187 (B/B Homodimerizer) (10nM),both, or neither for 8h. Cells are then rinsed with PBS and fixed with 4% paraformaldehyde for 1h at room temperature.After rinsing with PBS, cells are incubated in ice-cold permeabilization solution (0.1% Triton X-100, 0.1% sodium citrate) for 2 min at 0°C. Cells are rinsed with PBS and stained with TUNEL reaction mixture for 60 min at 37°C. After another PBS wash,cells are incubated with Converter-AP for 30min at 37°C. Cells are rinsed and incubated with substrate 5-bromo-4-chloro-3- indolyl phosphate/nitroblue tetrazolium for 30min. After a final PBS rinse (repeated twice), cells are microphotographed.

 

 

动物实验:

 

Animal Administration

To activate the transgene Fv2E-PERK in oligodendrocytes, PLP/Fv2E-PERK transgenic mice are given intraperitoneal injections of AP20187 (B/B Homodimerizer) daily at a dose of 0.5mg/kg, 2mg/kg, or 5mg/kg. Lyophilized AP20187 (B/B Homodimerizer) is dissolved in 100% ethanol at a concentration of 62.5mg/mL stock solution and stored at −20°C. Injection solutions consist of 4% ethanol, 10% PEG-400, and 2% Tween-20 in water. The transgenic mice receiving only the vehicle(4% ethanol, 10% PEG-400, 2% Tween-20 in water) served as controls.

保存条件:
-20℃
UN码:
HazardClass:
危害声明:
安全说明:
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参考文献 & 客户发表文献

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

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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

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    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
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    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):