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My CartCAS：124431-80-7
Storage：Powder:-20℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：White to off-white Solid
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| CAS | 124431-80-7 |
| Name | CGS-21680 Hydrochloride |
| Molecular Formula | C23H29N7O6·HCl |
| Molecular Weight | 535.98 |
| Solubility | Soluble in DMSO ≥5mg/mL |
| Purity | ≥98% |
| Appearance | White to off-white Solid |
| Storage | Powder:-20℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| MDL | MFCD00078573 |
| SMILES | O=C(O)CCC1=CC=C(CCNC2=NC3=C(N=CN3[C@H]4[C@H](O)[C@H](O)[C@@H](C(NCC)=O)O4)C(N)=N2)C=C1.Cl |
| Target Point | Adenosine Receptor |
| Passage | GPCR & G Protein |
| Background | CGS-21680 Hydrochloride is a selective adenosine A2A receptor agonist. |
| Biological Activity | CGS 21680 Hydrochloride是选择性的腺苷A2A受体激动剂，Ki为27 nM。[1-4] |
| In Vitro | CGS21680显著上调CD39和CD73表达。 CGS21680加速三磷酸腺苷(ATP)水解和腺苷生成[1]。单独的CGS21680(10nM)仅显示小的存活活性，但通过添加磷酸二酯酶抑制剂IBMX显著增强了活性。 CGS21680对培养的运动神经元的存活活性是通过腺苷酸环化酶-cAMP-PKA途径和神经营养素受体反式激活的混合作用发挥的[4]。 |
| In Vivo | CGS21680(1 mg / kg / ip)干预促进了EAN的发展。 CGS21680加剧了用牛外周髓鞘诱导的Lewis大鼠的实验性自身免疫性神经炎。恶化伴随着CD4 + Foxp3 + T细胞减少，CD4 + CXCR5 + T细胞，B细胞，树突细胞和抗原特异性自身抗体增加，这可能是由于CGS21680诱导的IL-2的抑制[2]。 CGS21680(0.1mg / kg，ip)短暂地增加心脏频率但不改变大鼠的血压，并且不改变心脏频率或0.01mg / kg的血压。在瞬时MCAo后，两种剂量的CGS21680从第一天到第7天保护免于神经缺陷。此时，它减少了小神经胶质细胞增生，星形胶质细胞增生和改善纹状体中的髓鞘组织和缺血皮质和纹状体的细胞结构。短暂MCAo后两天，CGS21680减少了浸润的粒细胞进入缺血组织的数量[3]。 |
| Cell Experiment | 将来自每组的10×106个MNC再悬浮于2mL RPMI 1640中。向细胞悬浮液中加入羧基荧光素二乙酸酯，琥珀酰亚胺酯(CFSE，终浓度2.5μM)并充分混合。在37℃下在黑暗中温育15分钟后，通过加入10mL冰冷的完全RPMI 1640(含有10％FBS)淬灭染色过程，并在冰上温育5分钟。然后用RPMI 1640洗涤细胞两次。将细胞沉淀重悬于完全RPMI 1640(含有10％FBS)中。将染色的MNC(1×10 6个细胞/ mL，1mL /孔)在24孔培养板中在黑暗中于37℃一式三份培养。向每个孔提供50μL伴刀豆球蛋白A(ConA，终浓度5μg/ mL)或50μLP0肽(终浓度10μg/ mL)。 72小时后，收集细胞并用PE标记的抗大鼠CD4抗体在4℃下染色30分钟。最后，用流式细胞仪分析细胞。 |
| Animal Experiment | 将6-8周龄的雌性Lewis大鼠(体重，140-160g)饲养在当地动物设施中的无特定病原体的条件下，自由获取水和食物。在第5天开始给予CGS21680(在PBS中以1mg / kg的剂量)。实验组中的大鼠每两天腹膜内(ip)注射CGS21680直至实验结束。对照组大鼠以相同方式给予等体积的PBS。测定剂量(1mg / kg / ip)和治疗方案(每两天，从第5天开始)。 |
| Data Literature Source | [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]. 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. [3]. 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. [4]. 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 |
| Unit | Bottle |
| Specification | 5mg 10mg |
是选择性的 adenosine A2A receptor 激动剂。
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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