中文名称: WIN552122 甲磺酸酯
英文名称: WIN552122 Mesylate
CAS No: 131543-23-2
分子式: C27H26N2O3.CH3SO3H
分子量: 522.61
W10006 WIN552122 甲磺酸酯 ≥98%(HPLC) (psaitong)
包装规格:
5mg 25mg 100mg in glass bottle
溶解性:
溶于DMSO(12mg/mL)。
产品描述:

基本信息

产品编号:W10006

产品名称:WIN552122 Mesylate

CAS:

131543-23-2

 

储存条件

粉末

-20℃

四年

 

 

分子式:

C27H26N2O3.CH3SO3H

溶于液体

-80℃

六个月

分子量:

522.61

-20℃

一个月

化学名: 

 

 

Solubility (25°C)

 

体外

DMSO

100mg/mL (191.34mM)

Ethanol

20mg/mL (38.26mM)

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

1.9135mL

9.5674mL

19.1347mL

5mM

0.3827mL

1.9135mL

3.8269mL

10mM

0.1913mL

0.9567mL

1.9135mL

50mM

0.0383mL

0.1913mL

0.3827mL

 

生物活性

产品描述

一种cb1(大麻素受体)激动剂.

靶点/IC50

CB2 
(Cell-free assay)

CB1
(Cell-free assay)

3.3nM(Ki)

62.3nM(Ki)

 

体外研究

WIN 55,212-2 is more potent in CHO-CB2 cells than in CHO-CB1 cells by a factor of 6O.WIN 55,212-2 has no effect on arachidonic acid release in CHO-CB2 or control CHO cells.WIN 55,212-2 fails to stimulate any increase in intracellular Ca2+up to 10μM.In primary cultures of rat cerebral cortex neurons,WIN 55,212-2 (0.01--100nM) increases extracellular glutamate levels,displaying a bell-shaped concentration-response curve.The facilitatory effect of WIN 55,212-2 (1nM) is fully counteracted by SR141716A (10nM),by the replacement of the normal Krebs Ringer-bicarbonate buffer with a low Ca2+medium (0.2mM) and by the IP receptor antagonist xestospongin C (1μM).WIN 55,212-2 evokes CGRP release from TG neurons in vitro (EC50=26μM) in a concentration- and calcium-dependent manner.WIN 55,212-2-2 neither inhibits capsaicinevokes CGRP release nor does it inhibit forskolin-,isoproteranol-or prostaglandin E2-stimulated cAMP accumulation.WIN 55,212-2 significantly inhibits (EC50=1.7μM) 50mm K+-evoked CGRP release by approximately 70%.WIN 55,212-2 inhibition of 50mm K+-evoked CGRP release is not reversed by antagonists of cannabinoid type 1 (CB1) receptor,but is mimicks in magnitude and potency (EC50=2.7μM) by its cannabinoid-inactive enantiomer WIN 55,212-2-3.

体内研究

In the prefrontal cortex WIN 55,212-2 (0.1 and 1mg/kg i.p.) increases dialysate glutamate levels from of the awake rat,while the lower (0.01mg/kg) and the higher (2mg/kg) doses are ineffective.Furthermore,the WIN 55,212-2 (0.1mg/kg)-induced increase of dialysate glutamate levels is counteracted by pretreatment with the selective CB receptor antagonist SR141716A (0.1mg/kg,i.p.) and by the local perfusion with a low-calcium Ringer solution (Ca2+0.2mM).WIN 55,212-2 (0.5,1,3,5,10 and 15mg/kg,i.p.) does not alter the seizure threshold at low doses,while higher doses of the drug significantly increases the threshold in a dose-dependent manner.The anticonvulsant effect of WIN 55,212-2,which is observed with doses as high as 5mg/kg,can be observed with doses as low as 0.5mg/kg in groups pre-treated with 20mg/kg of pioglitazone.

 

推荐实验方法(仅供参考)

动物实验:

 

In experiment 1,different doses of WIN 55,212-2 (0.5,1,3,5,10 and 15mg/kg) are injected 60 min prior to the determination of clonic seizure threshold induced by intravenous administration of PTZ solution.Control animals receive the same volume of the vehicle (1% aqueous solution of DMSO).The doses and time point are chosen on the basis of pilot studies.In experiment 2,in order to confirm the anticonvulsant effects of pioglitazone,different doses (10,20,40 and 80mg/kg) are administered 4h prior to PTZ in distinct groups of mice.The corresponding control groupreceive the appropriate vehicle (CMC 1%) at the same time point.In experiment 3,The additive anti epileptic effects of WIN 55,212-2 and pioglitazone are examined;mice receive acute administration of pioglitazone (10 or 20mg/kg) 3h before WIN 55,212-2 (0.5 or 1mg/kg) and 4h before PTZ.

保存条件:
-20℃
UN码:
HazardClass:
危害声明:
安全说明:
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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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    *
    *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

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  • 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):