中文名称: 瑞沙托维
英文名称: Resatorvid
CAS No: 243984-11-4
分子式: C15H17ClFNO4S
分子量: 361.82
R10252 瑞沙托维 ≥98% (psaitong)
包装规格:
5mg 10mg 25mg 50mg 100mg in glass bottle
溶解性:
溶于DMSO(100 mg/mL 超声)
产品描述:

基本信息

产品编号:

R10252

产品名称:

Resatorvid

CAS:

243984-11-4

 

储存条件

粉末

-20℃

四年

 

 

分子式:

C15H17ClFNO4S

溶于液体

-80℃

6个月

分子量:

361.82

-20℃

1个月

化学名: 

(6R)-6-[[(2-Chloro-4-fluorophenyl)amino]sulfonyl]-1-cyclohexene-1-carboxylic acid ethyl ester;TAK-242

Solubility (25°C):

 

体外:

 

DMSO

72mg/mL (198.99mM)

Ethanol

72mg/mL (198.99mM)

Water

Insoluble

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

2.7638mL

13.8190mL

27.6381mL

5mM

0.5528mL

2.7638mL

5.5276mL

10mM

0.2764mL

1.3819mL

2.7638mL

50mM

0.0553mL

0.2764mL

0.5528mL

 

生物活性

产品描述

一种选择性的TLR4信号传导抑制剂。Resatorvid抑制NO,TNF-α和IL-6的产生,其IC50值分别为1.8nM,1.9nM,1.3nM。

靶点

TLR4

IL-6 
(Cell-free assay)

NO 
(Cell-free assay)

TNF-α 
(Cell-free assay)

 

1.3nM

1.8nM

1.9nM

 

体外研究

Resatorvid suppresses the production of NO,TNF-α,and IL-6 from LPS-stimulated human peripheral blood mononuclear cells (PBMCs) at IC50 values from 11 to 33nM.Resatorvid (1-100nM;4 hours) inhibits mRNA expression of IL-6 and TNF-α induced by LPS and IFN-γ in RAW264.7 cells.Resatorvid (1-100nM;15 minutes;PBMCs cells) markedly inhibits the LPS-induced phosphorylation of extracellular signalregulated kinase 1/2 (Erk1/2),p38,and JNK/SAPK as well as degradation of IκBβ at a concentration of 100nM.

RT-PCR

Cell Line:

RAW264.7 cells

Concentration:

1nM,10nM,100nM

Incubation Time:

4 hours

Result:

TNF-α and IL-6 mRNA expression levels were clearly suppressed at concentrations of 10 to 100nM.

Western Blot Analysis

Cell Line:

PBMCs cells

Concentration:

1nM,10nM,100nM

Incubation Time:

15 minutes

Result:

The phosphorylation of mitogen-activated protein kinases induced by LPS was also inhibited in a concentration-dependent manner.

体内研究

Resatorvid (TAK-242;3mg/kg;intraperitoneal injection;for 2 days;male C57BL/6 mice) pretreatment markedly and significantly reverses the LPS-induced body weight loss,TA muscle loss,and muscle strength loss.TAK-242 reverses the LPSinduced shrinkage of muscle fibres and increases the interstitial space.TAK-242 blocks systemic catabolic cytokine release and skeletal muscle proteolysis in LPS-administered mice.

Animal Model:

Male C57BL/6 mice (8-12 weeks of age) treated with lipopolysaccharide (LPS).

Dosage:

3mg/kg

Administration:

Intraperitoneal injection;for 2 days

Result:

Pretreatment of mice reduced or reversed all the detrimental effects of LPS.

 

推荐实验方法(仅供参考)

细胞实验:

 

细胞系

原代角质形成细胞

浓度

10µM

处理时间

6h

方法

用紫外线照射NF-κB角质细胞,10µM resatorvid(或vehicle)处理6小时后,收集细胞。Resatorvid可显著地抑制紫外线诱导的NF-κB荧光素酶信号。

 

动物实验:

 

动物模型

4-5周龄的雄性ddY小鼠

剂量

1μl (at 0.001,0.03,or 0.01μg/μl)

给药处理

侧脑室注射

保存条件:
-20℃
UN码:
HazardClass:
危害声明:
安全说明:
搜索质检报告(COA)
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

  • =
    *
    *
    *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):