GlpBio

WIN 55,212-2 Mesylate

目录号: GC37935纯度: >98.00%同义词: (R)-(+)-WIN55,212-2甲磺酸盐,(R)-(+)-WIN 55212
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。
WIN 55,212-2 Mesylate
Cas No.: 131543-23-2
规格价格库存数量操作
5mg¥826.00现货
1
10mg¥1,568.00现货
1
25mg¥3,514.00现货
1
50mg¥6,202.00现货
1
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产品描述 Description

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 WIN55,2122 mesylate inhibits ADAMTS4 activity in human osteoarthritic articular chondrocytes by inhibiting expression of syndecan1[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]。

实验参考方法 Experimental Reference Method

Cell experiment [1]:

Cell lines

Dorsal root ganglion (DRG) neurons

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.

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]:

Animal models

Swiss mice

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:
[1]Tan R, Cao L. Cannabinoid WIN-55,212-2 mesylate inhibits tumor necrosis factor-?-induced expression of nitric oxide synthase in dorsal root ganglion neurons[J]. International Journal of Molecular Medicine, 2018, 42(2): 919-925.
[2]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).

产品文档 Product Documents

Purity:>98.00%

化学性质Chemical Properties

CAS 号
131543-23-2
同义词
(R)-(+)-WIN55,212-2甲磺酸盐,(R)-(+)-WIN 55212
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 g/mol
溶解性
DMSO: ≥ 34 mg/mL (65.06 mM)
保存条件
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°C，然后在超声波浴中震荡一段时间。
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。

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