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Submit Review(±)-5'-Chloro-5'-deoxy-ENBA is a highly selective adenosine A1 receptor agonist (Ki values are 0.51, 1290, 1340 and 2740 nM at A1, A3, A2A and A2B receptors respectively). Reverses formalin-induced nocifensive behavior in mice; antinociceptive.
(±)-5'-Chloro-5'-deoxy-ENBA is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
分子量 | 379.84 |
公式 | C17H22ClN5O3 |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 103626-26-2 |
PubChem ID | 42636897 |
InChI Key | PVJGDYDNVNCGBT-STHLEMNDSA-N |
Smiles | O[C@@H]1[C@H](O)[C@@H](CCl)O[C@H]1N(C=N3)C2=C3C(NC4C5CCC(C5)C4)=NC=N2 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 37.98 | 100 | |
ethanol | 37.98 | 100 |
以下数据基于产品分子量 379.84。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 2.63 mL | 13.16 mL | 26.33 mL |
5 mM | 0.53 mL | 2.63 mL | 5.27 mL |
10 mM | 0.26 mL | 1.32 mL | 2.63 mL |
50 mM | 0.05 mL | 0.26 mL | 0.53 mL |
参考文献是支持产品生物活性的出版物。
Trivedi et al (1989) N6-bicycloalkyladenosines with unusually high potency and selectivity for the adenosine A1 receptor. J.Med.Chem. 32 8 PMID: 2909748
Franchetti et al (2009) N6-cycloalkyl- and N6-bicycloalkyl-C5'(C2')-modified adenosine derivatives as high-affinity and selective agonists at the human A1 adenosine receptor with antinociceptive effects in mice. J.Med.Chem. 52 2393 PMID: 19317449
If you know of a relevant reference for (±)-5'-Chloro-5'-deoxy-ENBA, please let us know.
关键词: (±)-5'-Chloro-5'-deoxy-ENBA, (±)-5'-Chloro-5'-deoxy-ENBA supplier, highly, selective, A1, adenosines, receptors, agonists, (±)-5-Chloro-5-deoxy-ENBA, ENBA, Adenosine, Receptors, 3576, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 (±)-5'-Chloro-5'-deoxy-ENBA 的部分引用包括:
Cuiying et al (2020) Activation of neuronal adenosine A1 receptors causes hypothermia through central and peripheral mechanisms. PLoS One 15 e0243986 PMID: 33326493
Wei et al (2021) Adenosine A2A Receptor Activation Enhances Blood-Tumor Barrier Permeability in a Rodent Glioma Model. Mol Cancer Res 19 2081-2095 PMID: 34521765
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平均评分: 5 (Based on 1 Review.)
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In the first work, we demonstrated that chronic systemic administration of 5′-chloro-5′-deoxy-(±)-ENBA (0.5 mg/kg, i.p.) reduced both mechanical allodynia and thermal hyperalgesia 3 and 7 days post-SNI, in a way prevented by DPCPX (3 mg/kg, i.p.), a selective A1 adenosine receptor antagonist, without exerting any significant change on the motor coordination or arterial blood pressure (Molecules. 2012, 17, 13712-13726. doi: 10.3390/molecules171213712).Then, the product has been used to clearly demonstrate that functionalA1ARs are expressed in microglia (Glia. 2014, 62,122-132. doi: 10.1002/glia.22592).In addition, we found that 5′Cl5′ d-(±)-ENBA, administered in combination with L-DOPA, reduced the development of abnormal involuntary movements. These results indicate the potential benefit of A1R agonists for the treatment of L-DOPA-induced dyskinesia and hyperkinetic disorders providing a mechanistic framework for the study of the interaction between DA and adenosine in the striatonigral system (Exp Neurol. 2014, 261, 733-43. doi: 10.1016/j.expneurol.2014.08.022).
the product has to be stored in the refrigerator (-20°C) otherwise (room temperature) decompose