010-60605840
结构式搜索
  1. 首页
  2. 产品目录
  3. Signaling Pathways(信号通路)
  4. GPCR/G Protein
  5. Cannabinoid Receptor
中文名称: AM251
英文名称: AM251
CAS No: 183232-66-8
分子式: C22H21Cl2In4O
分子量: 555.24
安全技术说明书(PDF) MSDS(PDF) 点击下载产品说明书(PDF)
A11441 AM251 ≥98% (psaitong)
包装规格：
50mg in glass bottle
溶解性：
溶于DMSO（25mg/mL 超声）
产品描述：

基本信息

产品编号：

A11441

产品名称：

AM251

CAS:

183232-66-8

 

储存条件

粉末

-20℃

四年

 

 

分子式：

C22H21Cl2In4O

溶于液体

-80℃

6个月

分子量：

555.24

-20℃

1个月

化学名： 

1-(2,4-Dichlorophenyl)-5-(4-iodophenyl)-4-methyl-N-(piperidin-1-yl)-1H-pyrazole-3-carboxamide

Solubility (25°C)：

 

体外:

 

DMSO

40mg/mL (72.04mM)

Ethanol

Insoluble

Water

Insoluble

体内(现配现用):

5% DMSO+40% PEG 300+5% Tween 80+50% ddH2O

1mg/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

1.8010mL

9.0051mL

18.0102mL

5mM

0.3602mL

1.8010mL

3.6020mL

10mM

0.1801mL

0.9005mL

1.8010mL

50mM

0.0360mL

0.1801mL

0.3602mL

 

生物活性

产品描述

一种选择性大麻素1 (CB1)受体拮抗剂，IC50为8nM。AM25也是GPR55 的激动剂，EC50为39nM。

靶点

IC50:8nM (CB1 receptor)

 

体外研究

AM251 is a CB1 receptor antagonist/inverse agonist.AM251 produces an agonist response in HEK293 cells,similar to that found in the yeast expression system.AM-251 reduces cholesteryl ester synthesis in unstimulated and acetylated LDLstimulated Raw 264.7 macrophages,CB2+/+and CB2-/-peritoneal macrophages.

体内研究

The CB1 antagonist AM251 (3mg/kg,i.p.) decreases capsaicin-evoked nocifensive behavior (F1,18=28.45,p<0.0001).This suppressive effect is genotype dependent (F1,18=14.83,p<0.01),and the interaction between the effects of genotype and AM251 approached significance (F1,18=4.704,p=0.0587).Planned comparisons reveal that AM251 reduces nocifensive behaviors in fatty-acid amide hydrolase (FAAH) KO mice (p<0.01) but fails to alter nocifensive behavior in WT mice (p>0.2) relative to their respective vehicle controls. AM251 (3mg/kg,i.p.) reduces the duration of heat hypersensitivity in FAAH KO (F 1,9=21.43,p<0.01) but not WT mice (p>0.3).AM251 suppresses capsaicin-evoked heat hypersensitivity in a time-dependent manner in FAAH KO (F5,9=4.349,p<0.01) but not in WT mice (p>0.3).Post-hoc analysis reveals that FAAH KO mice receiving vehicle (i.p.) display heightened thermal hypersensitivity at 30 (p<0.05),60 (p<0.05),and 90 (p<0.001) minutes post-capsaicin in comparison to FAAH KO animals receiving AM251).One-way ANOVA shows that AM251 (AM-251) injected into the rats significantly decreases both of the percentage of entries in the open arms and time spent in the open arms,compare to controls.The Tukey-Kramer test analysis reveals a significant reduction for the doses of 1mg/kg (P<0.05) and 5mg/kg (P<0.01) compare to control rats in the time spent in the open arms.Also,AM251 significantly decreases percentage of entries in the open arms for the doses of 1 and 5mg/kg (P<0.05).

 

推荐实验方法(仅供参考)

激酶实验：

Macrophages are seeded (2×106/well) in 12-well culture plates.AM-251 or SR144528 are added from 4mM stock solutions prepared in DMSO,1h prior to the addition of 7-ketocholesterol (7KC) from a 2mg/mL ethanol stock solution.Controls are adjusted to receive equivalent volumes of DMSO and ethanol.After 16h,caspase-3 activity is determined. All treatments are done in triplicate and the data presented as the mean RFLU/mg protein±SD.

 

动物实验:

 

Mice

A total of 246 mice weighing 17-48g are used in these experiments.Following determination of baseline responding,mice receive a single i.p injection (5mL/kg) of AMG9810 (3mg/kg,n=5 per group),AM251 (3mg/kg,n=5 per group),or vehicle (n=6 per group).I.p.injections are performed 30 min prior to i.pl.capsaicin or vehicle administration.Paw withdrawal latencies are assessed before and 10,30,60,90 and 120 min after intradermal injection of capsaicin or vehicle.Paw withdrawal latencies are measured in duplicate in each paw at each time point,and are reported as the mean of the two duplicate determinations from each animal,averaged across subjects.

Rats

Male Wistar rats weighting 250-350 are used.The following agents are used:CB1 receptor agonist,Win-55212 (0.3,1 and 5mg/kg,i.p.);CB1 receptor antagonist,AM251 (0.3,1 and 5mg/kg,i.p.);endocannabinoid breakdown inhibitor,URB-597 (0.03,0.1 and 0.3mg/kg,i.p.) in the study.Physiological saline (0.9% sodium chloride) is used as the vehicle.All drugs are prepared freshly and administered intraperitoneally (i.p.) in a volume of 0.1mL per 10g of body weight of the rats.All substances are dissolved in physiological saline and are administrated 30 min before elevated plus-maze test.
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):
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