WIN 55,212-2 Mesylate
(Synonyms: (R)-(+)-WIN55,212-2甲磺酸盐,(R)-(+)-WIN 55212) 目录号 : GC37935
WIN 55,212-2 Mesylate是一种有效的氨烷基吲哚大麻素（CB）受体激动剂，对人类重组CB1和CB2受体的Ki值分别为62.3nM和3.3nM。
Cas No.:131543-23-2
Sample solution is provided at 25 µL, 10mM.
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WIN 55,212-2 Mesylate is a potent aminoalkylindole cannabinoid (CB) receptor agonist with Ki values of 62.3nM and 3.3nM for human recombinant CB1 and CB2 receptors, respectively[1]. WIN 55,212-2 Mesylate produces antinociceptive effects through a peripheral mechanism of action[2]. WIN 55,212-2 Mesylate has vasorelaxant effects[3].
In vitro, treatment of rat dorsal root ganglion (DRG) neurons with WIN 55,212-2 Mesylate (100-400ng/mL) for 25h abolished TNF-α-induced nNOS expression and inhibited p38 MAPK activity in DRG neurons in a concentration- and time-dependent manner[4]. WIN 55,212-2 Mesylate (0.5-8μM) treated primary human chondrocytes for 24h, concentration-dependently inhibited IL-1β-stimulated aggrecanase-1 (ADAMTS-4) activity and syndecan-1 protein expression levels, but not ADAMTS-4 protein expression levels[5].
In vivo, WIN 55,212-2 Mesylate (5-20mg/kg) treated Swiss mice by intraperitoneal injection increased the threshold of maximum electric shock (MEST)-induced epilepsy in a dose-dependent manner[6]. WIN 55,212-2 Mesylate (1.25-15mg/kg) treated Swiss mice by intraperitoneal injection, administered 20 minutes before the acute heat pain test, prolonged the latency of the mice's first pain response in a dose-dependent manner[7].
References:
[1] Felder C C, Joyce K E, Briley E M, et al. Comparison of the pharmacology and signal transduction of the human cannabinoid CB1 and CB2 receptors[J]. Molecular pharmacology, 1995, 48(3): 443-450.
[2] Price T J, Patwardhan A, Akopian A N, et al. Cannabinoid receptor‐independent actions of the aminoalkylindole WIN 55,212‐2 on trigeminal sensory neurons[J]. British journal of pharmacology, 2004, 142(2): 257-266.
[3] Dannert M T, Alsasua A, Herradon E, et al. Vasorelaxant effect of Win 55,212-2 in rat aorta: new mechanisms involved[J]. Vascular pharmacology, 2007, 46(1): 16-23.
[4] Tan R, Cao L. Cannabinoid WIN-55,212-2 mesylate inhibits tumor necrosis factor-α-induced expression of nitric oxide synthase in dorsal root ganglion neurons[J]. International Journal of Molecular Medicine, 2018, 42(2): 919-925.
[5] Kong Y, Wang W, Zhang C, et al. Cannabinoid WIN 55,212 2 mesylate inhibits ADAMTS 4 activity in human osteoarthritic articular chondrocytes by inhibiting expression of syndecan 1[J]. Molecular medicine reports, 2016, 13(6): 4569-4576.
[6] Luszczki J J, Misiuta-Krzesinska M, Wlaz A, et al. WIN 55,212-2 mesylate (a highly potent non-selective cannabinoid CB1 and CB2 receptor agonist) elevates the threshold for maximal electroshock-induced seizures in mice[J]. Journal of Pre-Clinical and Clinical Research, 2009, 3(2).
[7] Łuszczki J J, Florek-Łuszczki M. Synergistic interaction of pregabalin with the synthetic cannabinoid WIN 55,212-2 mesylate in the hot-plate test in mice: an isobolographic analysis[J]. Pharmacological Reports, 2012, 64(3): 723-732.
WIN 55,212-2 Mesylate是一种有效的氨烷基吲哚大麻素（CB）受体激动剂，对人类重组CB1和CB2受体的Ki值分别为62.3nM和3.3nM[1]。WIN 55,212-2 Mesylate可通过外周作用机制产生抗痛觉作用[2]。WIN 55,212-2 Mesylate具有血管松弛作用[3]。
在体外，WIN 55,212-2 Mesylate（100-400ng/mL）处理大鼠背根神经节（DRG）神经元25h，以浓度和时间依赖性方式消除了TNF-α诱导的nNOS表达，并抑制了DRG神经元p38 MAPK活性[4]。WIN 55,212-2 Mesylate（0.5-8μM）处理原代人软骨细胞24h，浓度依赖性地抑制了IL-1β刺激的聚集蛋白聚糖酶-1（ADAMTS-4）活性，抑制了复合蛋白聚糖-1（syndecan-1）的蛋白表达水平，但不抑制ADAMTS-4的蛋白表达水平[5]。
在体内，WIN 55,212-2 Mesylate（5-20mg/kg）通过腹腔注射处理Swiss小鼠，剂量依赖性地增加了最大电休克（MEST）诱发癫痫的阈值[6]。WIN 55,212-2 Mesylate（1.25-15mg/kg）通过腹腔注射处理Swiss小鼠，在急性热痛试验前20分钟给药，以剂量依赖性方式延长了小鼠首次疼痛反应的潜伏期[7]。
| Cell experiment [1]: | |
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Cell lines |
Dorsal root ganglion (DRG) neurons |
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Preparation Method |
DRG neurons were treated with TNF-α (40ng/mL) in the presence of WIN 55,212-2 Mesylate (100, 200, 300 and 400ng/mL) for 1, 5, 10, 15, 20 and 25h. Cells treated with TNF-α only were used as a control. The nNOS mRNA levels was measured and expressed as fold-changes to that of untreated cells. |
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Reaction Conditions |
100, 200, 300 and 400ng/mL; |
|
Applications |
In DRG neurons treated with TNF-α, WIN 55,212-2 Mesylate concentration- and time-dependently abolished TNF-α-induced expression of nNOS. |
| Animal experiment [2]: | |
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Animal models |
Swiss mice |
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Preparation Method |
Electroconvulsions were induced in mice by electric current (sinusoidal wave, 50Hz, maximum 500V, intensity 4-14mA, through ear-clip electrodes, stimulation duration 0.2s, end point in tonic hindlimb extension). Four groups of animals were intraperitoneally injected with WIN 55,212-2 Mesylate at doses of 5, 10, 15, and 20mg/kg 20 min before the maximum electroshock (MEST) test, and the maximum electroshock threshold was recorded. |
|
Dosage form |
5, 10, 15, 20mg/kg; i.p. |
|
Applications |
WIN 55,212-2 Mesylate dose-dependently increases the threshold for MEST-induced seizures. |
|
References: |
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| Cas No. | 131543-23-2 | SDF | |
| 别名 | (R)-(+)-WIN55,212-2甲磺酸盐,(R)-(+)-WIN 55212 | ||
| Canonical SMILES | O=C(C1=C2C=CC=CC2=CC=C1)C3=C(N4[C@@H](COC5=C4C3=CC=C5)CN6CCOCC6)C.CS(=O)(O)=O | ||
| 分子式 | C28H30N2O6S | 分子量 | 522.61 |
| 溶解度 | DMSO: ≥ 34 mg/mL (65.06 mM) | 储存条件 | Store at -20°C |
| General tips | 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。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.9135 mL | 9.5674 mL | 19.1347 mL |
| 5 mM | 0.3827 mL | 1.9135 mL | 3.8269 mL |
| 10 mM | 0.1913 mL | 0.9567 mL | 1.9135 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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