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Submit ReviewNECA is a high affinity adenosine receptor agonist (Ki values are 6.2, 14, and 20 nM for human A3, A1 and A2A receptors respectively; EC50 = 2.4 μM for human A2B). Inhibits platelet aggregation and is centrally active in vivo.
NECA 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 | 308.3 |
公式 | C12H16N6O4 |
储存 | Store at +4°C |
纯度 | ≥98% (HPLC) |
CAS Number | 35920-39-9 |
PubChem ID | 448222 |
InChI Key | JADDQZYHOWSFJD-FLNNQWSLSA-N |
Smiles | O[C@@H]1[C@@H]([C@](NCC)=O)O[C@@H](N2C=NC3=C2N=CN=C3N)[C@@H]1O |
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 | 12.33 | 40 |
以下数据基于产品分子量 308.3。 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 |
---|---|---|---|
0.4 mM | 8.11 mL | 40.54 mL | 81.09 mL |
2 mM | 1.62 mL | 8.11 mL | 16.22 mL |
4 mM | 0.81 mL | 4.05 mL | 8.11 mL |
20 mM | 0.16 mL | 0.81 mL | 1.62 mL |
参考文献是支持产品生物活性的出版物。
Cusack and Hourani (1981) 5'-N-ethylcarboxamidoadenosine: a potent inhibitor of human platelet aggregation. Br.J.Pharmacol. 72 443 PMID: 7260485
Klotz (2000) Adenosine receptors and their ligands. Naunyn Schmiedebergs Arch.Pharmacol. 362 382 PMID: 11111832
Knapp et al (2001) Adenosine agonists CGS21680 and NECA inhibit the initiation of cocaine self-administration. Pharmacol.Biochem.Behav. 68 797 PMID: 11526979
If you know of a relevant reference for NECA, please let us know.
关键词: NECA, NECA supplier, adenosines, receptor, agonists, Non-Selective, Receptors, 5-N-Ethylcarboxamidoadenosine, 5'-N-Ethylcarboxamidoadenosine, Non-selective, Adenosine, 1691, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 NECA 的部分引用包括:
Kinsey et al (2012) Autocrine adenosine signaling promotes regulatory T cell-mediated renal protection. J Am Soc Nephrol 23 1528 PMID: 22835488
Garavaglia et al (2010) Adaptation of NS cells growth and differentiation to high-throughput screening-compatible plates. BMC Neurosci 11 7 PMID: 20085655
Jin et al (2010) CD73 on tumor cells impairs antitumor T-cell responses: a novel mechanism of tumor-induced immune suppression. Cancer Res 70 2245 PMID: 20179192
Liu et al (2018) Adenosine binds predominantly to adenosine receptor A1 subtype in astrocytes and mediates an immunosuppressive effect. Brain Res 1700 47 PMID: 29935155
Bertheleme et al (2014) Arginine 199 and leucine 208 have key roles in the control of adenosine A2A receptor signalling function. PLoS One 9 e89613 PMID: 24595172
Pedroza et al (2011) Interleukin-6 contributes to inflammation and remodeling in a model of adenosine mediated lung injury. J Clin Immunol 6 e22667 PMID: 21799929
Gomez et al (2011) Disparity in FcηRI-induced degranulation of primary human lung and skin mast cells exposed to adenosine. Nature 31 479 PMID: 21437670
Klysz et al (2024) Inosine induces stemness features in CAR-T cells and enhances potency. Cancer Cell 42 266 PMID: 38278150
Salimu et al (2017) Dominant immunosuppression of dendritic cell function by prostate-cancer-derived exosomes. J Extracell Vesicles 6 1368823 PMID: 28959385
Al-Taei et al (2017) Prostaglandin E2-mediated adenosinergic effects on CD14+ cells: Self-amplifying immunosuppression in cancer. Oncoimmunology 6 e1268308 PMID: 28344879
Poddar et al (2014) Enhanced brain distribution of modified aspartoacylase. Mol Genet Metab 113 219 PMID: 25066302
Welihinda and Amento (2014) Positive allosteric modulation of the adenosine A2a receptor attenuates inflammation. J Inflamm (Lond) 11 37 PMID: 25473378
Aggarwal et al (2013) Macrophage A2A adenosinergic receptor modulates oxygen-induced augmentation of murine lung injury. PLoS One 48 635 PMID: 23349051
Mahamed et al (2015) CD73-generated adenosine is critical for immune regulation during Toxoplasma gondii infection. Infect Immun 83 721 PMID: 25452548
Kim and Bynoe (2015) A2A Adenosine Receptor Regulates the Human Blood-Brain Barrier Permeability. Am J Respir Cell Mol Biol 52 664 PMID: 25262373
Bulavina et al (2013) NTPDase1 activity attenuates microglial phagocytosis. Purinergic Signal 9 199 PMID: 23208703
Carman et al (2011) Adenosine receptor signaling modulates permeability of the blood-brain barrier. J Neurosci 31 13272 PMID: 21917810
Akoume et al (2019) A Differential Hypofunctionality of Gαi Proteins Occurs in Adolescent Idiopathic Scoliosis and Correlates with the Risk of Disease Progression. Sci Rep 9 10074 PMID: 31296888
Song (2017) Erythrocytes retain hypoxic adenosine response for faster acclimatization upon re-ascent. Nat Commun 8 14108 PMID: 28169986
Xi et al (2009) Adenosine A2A and A2B receptors work in concert to induce a strong protection against reperfusion injury in rat hearts. J Mol Cell Cardiol 47 684 PMID: 19695259
Clark et al (2009) Adenosine-evoked hyperpolarization of retinal ganglion cells is mediated by G-protein-coupled inwardly rectifying K+ and small conductance Ca2+-activated K+ channel activation. J Neurosci 29 11237 PMID: 19741130
Kim and Bynoe (2016) A2A adenosine receptor modulates drug efflux transporter P-glycoprotein at the blood-brain barrier. J Clin Invest 126 1717 PMID: 27043281
Schulz et al (2016) Critical role for adenosine receptor A2a in β-cell proliferation. Mol Metab 5 1138 PMID: 27818940
Newman (2005) Calcium increases in retinal glial cells evoked by light-induced neuronal activity. Mol Neurobiol 25 5502 PMID: 15944378
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HEK-A2AR cell lines (BPSBioscience) were treated with Forskolin, NECA, and CGS for 30 minutes and level of cAMP was measured.
0.08 mg/kg of NECA