MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。

WIN 55,212-2 Mesylate

CAS No. : 131543-23-2

MCE 站：WIN 55,212-2 Mesylate

产品活性：WIN 55,212-2 Mesylate 是一种有效的 cannabinoid receptor 激动剂，对人重组 CB1 和 CB2 受体的K_i 值分别为 62.3 和 3.3 nM。

研究领域：GPCR/G Protein  |  Neuronal Signaling

作用靶点：Cannabinoid Receptor

In Vitro: 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 10 μM. In primary cultures of rat cerebral cortex neurons, WIN 55,212-2 (0.01--100 nM) increases extracellular glutamate levels, displaying a bell-shaped concentration-response curve. The facilitatory effect of WIN 55,212-2 (1 nM) is fully counteracted by SR141716A (10 nM), by the replacement of the normal Krebs Ringer-bicarbonate buffer with a low Ca²⁺ medium (0.2 mM) and by the IP(3) receptor antagonist xestospongin C (1 μM). WIN 55,212-2 evokes CGRP release from TG neurons in vitro (EC₅₀=26 μM) in a concentration- and calcium-dependent manner. WIN 55,212-2-2 neither inhibits capsaicin-evokes CGRP release nor does it inhibit forskolin-, isoproteranol- or prostaglandin E2-stimulated cAMP accumulation. WIN 55,212-2 significantly inhibits (EC₅₀=1.7 μM) 50 mm K⁺-evoked CGRP release by approximately 70%. WIN 55,212-2 inhibition of 50 mm K⁺-evoked CGRP release is not reversed by antagonists of cannabinoid type 1 (CB1) receptor, but is mimicks in magnitude and potency (EC₅₀=2.7 μM) by its cannabinoid-inactive enantiomer WIN 55,212-2-3.

In Vivo: In the prefrontal cortex WIN 55,212-2 (0.1 and 1 mg/kg i.p.) increases dialysate glutamate levels from of the awake rat, while the lower (0.01 mg/kg) and the higher (2 mg/kg) doses are ineffective. Furthermore, the WIN 55,212-2 (0.1 mg/kg)- induced increase of dialysate glutamate levels is counteracted by pretreatment with the selective CB(1) receptor antagonist SR141716A (0.1 mg/kg, i.p.) and by the local perfusion with a low-calcium Ringer solution (Ca²⁺ 0.2 mM). WIN 55,212-2 (0.5, 1, 3, 5, 10 and 15 mg/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 5 mg/kg, can be observed with doses as low as 0.5 mg/kg in groups pre-treated with 20 mg/kg of pioglitazone.

相关产品：Bioactive Compound Library Plus  |  GPCR/G Protein Compound Library  |  Neuronal Signaling Compound Library  |  Rimonabant Hydrochloride  |  AM251  |  JD-5037  |  SR144528  |  2-Arachidonoylglycerol  |  6-Iodopravadoline  |  Pregnenolone  |  β-Caryophyllene  |  Olivetol  |  Olorinab  |  N-Oleoyl glycine  |  Org 27569  |  CB1 antagonist 2  |  TM38837  |  Yangonin  |  Taranabant ((1R,2R)stereoisomer)  |  MDA 19  |  BML-190  |  2-Palmitoylglycerol  |  AM281  |  BAY 38-7271  |  CB2R PAM  |  Hemopressin (human, mouse)  |  Hemopressin(rat)  |  Leelamine hydrochloride

品牌介绍:
•   MCE (MedChemExpress) 拥有数百种全球独家化合物，我们致力于为全球科研客户提供*新*全的高品质小分子活性化合物；
•   10,000 多种高选择性抑制剂、激动剂涉及各热门信号通路及疾病领域；
•   设有专业的实验中心和严格的质控、验证体系；
•   提供 LC/MS、NMR、HPLC、手性分析、元素分析等各项质检报告，确保产品的高纯度、高品质；
•   产品的生物活性多经各国客户实验验证；
•   Nature, Cell, Science 等多种期刊及制药收录了MCE客户的科研成果；
•   专业团队跟踪*新的制药及生命科学研究进展，为您提供全球*新的活性化合物；
•   与世界各大制药公司及知名科研机构建立了长期的合作。