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产品描述： CGS 21680 Hydrochloride is a selective adenosine A2A receptor agonist with a Ki of 27 nM. |
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靶点：
Ki: 27 nM (Adenosine A2A receptor);AdenosineReceptor |
体内研究：
CGS21680 (1 mg/kg/i.p.) intervention promotes the development of EAN. CGS21680 exacerbates experimental autoimmune neuritis in Lewis rats induced with bovine peripheral myelin. The exacerbation is accompanied with reduced CD4+ Foxp3+ T cells, increased CD4+ CXCR5+ T cells, B cells, dendritic cells and antigen-specific autoantibodies, which is possibly due to the inhibition of IL-2 induced by CGS21680. CGS21680 (0.1 mg/kg, i.p.) transiently increases heart frequency but does not modify blood pressure of rat, and does not modify either heart frequency or blood pressure at 0.01 mg/kg. Following transient MCAo, CGS21680 at both doses protects from neurological deficit from the first day up to 7 days thereafter. At this time, it has reduced microgliosis, astrogliosis and improved myelin organization in the striatum and cytoarchitecture of the ischemic cortex and striatum. Two days after transient MCAo, CGS21680 has reduced the number of infiltrated granulocytes into the ischemic tissue |
参考文献：
1. Bao R, et al. Adenosine and the adenosine A2A receptor agonist, CGS21680, upregulate CD39 and CD73 expression through E2F-1 and CREB in regulatory T cells isolated from septic mice. Int J Mol Med. 2016 Sep;38(3):969-75. 2. Komaki S, et al. Trk and cAMP-dependent survival activity of adenosine A(2A) agonist CGS21680 on rat motoneurons in culture. Neurosci Lett. 2012 Jul 26;522(1):21-4. 3. Zhang M, et al. Activation of the adenosine A2A receptor exacerbates experimental autoimmune neuritis in Lewis rats in association with enhanced humoral immunity. J Neuroimmunol. 2016 Apr 15;293:129-36. 4. Rosaria Volpini, et al. Adenosine receptor agonists: synthesis and binding affinity of 2-(aryl)alkylthioadenosine derivatives. 5. Melani A, et al. Low doses of the selective adenosine A2A receptor agonist CGS21680 are protective in a rat model of transient cerebral ischemia. Brain Res. 2014 Mar 10;1551:59-72. |
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溶解性：
DMSO : ≥ 20 mg/mL (37.31 mM) H2O : < 0.1 mg/mL (insoluble) |
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保存条件：
2-8℃ |
配置溶液浓度参考：
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1mg |
5mg |
10mg |
| 1 mM |
1.866 ml |
9.329 ml |
18.657 ml |
| 5 mM |
0.373 ml |
1.866 ml |
3.731 ml |
| 10 mM |
0.187 ml |
0.933 ml |
1.866 ml |
| 50 mM |
0.037 ml |
0.187 ml |
0.373 ml |
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| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
北京