中文名称: | WIN552122 甲磺酸酯 | ||||
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英文名称: | WIN552122 Mesylate | ||||
CAS No: | 131543-23-2 | 分子式: | C27H26N2O3.CH3SO3H | 分子量: | 522.61 |
CAS No: | 131543-23-2 | ||||
分子式: | C27H26N2O3.CH3SO3H | ||||
分子量: | 522.61 |
基本信息
产品编号:W10006 |
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产品名称:WIN552122 Mesylate |
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CAS: |
131543-23-2 |
储存条件 |
粉末 |
-20℃ |
四年 |
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分子式: |
溶于液体 |
-80℃ |
六个月 |
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分子量: |
522.61 |
-20℃ |
一个月 |
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化学名: |
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Solubility (25°C) |
体外 |
DMSO |
100mg/mL (191.34mM) |
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Ethanol |
20mg/mL (38.26mM) |
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Water |
Insoluble |
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体内(现配现用) |
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<1mg/ml表示微溶或不溶。 |
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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。 |
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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. |
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靶点/IC50 |
CB2 |
CB1 |
3.3nM(Ki) |
62.3nM(Ki) |
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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. |
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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: |
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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. |
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
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 )