NECA
(Synonyms: 5'-N-乙基酰胺基腺苷,NECA) 目录号 : GC15304
NECA是一种非选择性腺苷受体激动剂。
Cas No.:35920-39-9
Sample solution is provided at 25 µL, 10mM.
NECA is a non-selective agonist of adenosine receptors [1]. NECA regulates intracellular cAMP levels by activating adenosine receptors, thereby affecting many cellular physiological processes, such as anti-inflammation, vasodilation, inhibition of neuronal activity, cardioprotection, and immune regulation [2-3].
In H9c2 cells, NECA (0.1–10μM; 20min) blocked H2O2-induced GSK-3β phosphorylation and GRP94 expression [4]. In skeletal muscle cells, NECA (100nM, 10μM; 19h) modulates CPT1B, stimulates LCAD, inhibits ACCβ mRNA gene expression [5]. In HREC cells, NECA (10μM; 24-72h) induced a time-dependent increase in cell proliferation [6].
In ex-hypoxic polycythemic mice model, NECA (0.05, 0.1µmol/kg; iv; single injection) significantly increased serum erythropoietin levels in mice with hypoxic erythrocytosis [7]. In mice that were only immunized, intranasal NECA (50μL; 1mM; intranasal administration; single administration) administration caused a significant increase in bronchoalveolar lavage total cell count (TCC), neutrophils and eosinophils [8].
References:
[1]. Knapp C M, Foye M M, Cottam N, et al. Adenosine agonists CGS 21680 and NECA inhibit the initiation of cocaine self-administration[J]. Pharmacology Biochemistry and Behavior, 2001, 68(4): 797-803.
[2]. Elsherbiny N M, Abd El Galil K H, Gabr M M, et al. Reno-protective effect of NECA in diabetic nephropathy: implication of IL-18 and ICAM-1[J]. European Cytokine Network, 2012, 23(3): 78-86.
[3]. Li L, Chen J, Wang Z, et al. NECA alleviates inflammatory responses in diabetic retinopathy through dendritic cell toll-like receptor signaling pathway[J]. Frontiers in Immunology, 2024, 15: 1415004.
[4]. Xing F, Han H, He Y, et al. Roles of endoplasmic reticulum stress in NECA‐induced cardioprotection against ischemia/reperfusion injury[J]. Oxidative Medicine and Cellular Longevity, 2017, 2017(1): 2490501.
[5]. Haddad M. The effect of NECA, CGS 21680, PSB 603 on fatty acid transport and oxidation in skeletal muscle cells[J]. International Journal of Pharmaceutical Sciences and Research, 2016, 7(12): 4827.
[6]. Grant M B, Davis M I, Caballero S, et al. Proliferation, migration, and ERK activation in human retinal endothelial cells through A2B adenosine receptor stimulation[J]. Investigative ophthalmology & visual science, 2001, 42(9): 2068-2073.
[7]. Nakashima J, Ohigashi T, Brookins J W, et al. Effects of 5′-N-ethylcarboxamideadenosine (NECA) on erythropoietin production[J]. Kidney international, 1993, 44(4): 734-740.
[8]. El-Hashim A Z, Abduo H T, Rachid O M, et al. Intranasal administration of NECA can induce both anti-inflammatory and pro-inflammatory effects in BALB/c mice: Evidence for A2A receptor sub-type mediation of NECA-induced anti-inflammatory effects[J]. Pulmonary Pharmacology & Therapeutics, 2009, 22(3): 243-252.
NECA是一种非选择性腺苷受体激动剂 [1]。NECA通过激活腺苷受体调节细胞内cAMP水平，从而影响多种细胞生理过程，例如抗炎、血管舒张、抑制神经元活动、心脏保护和免疫调节 [2-3]。
在H9c2细胞中，NECA（0.1-10μM；20分钟）可阻断H2O2诱导的GSK-3β磷酸化和GRP94表达 [4]。在骨骼肌细胞中，NECA（100nM，10μM；19h）可调节CPT1B，刺激LCAD，并抑制ACCβ mRNA基因表达 [5]。在HREC细胞中，NECA（10μM；24-72h）可诱导细胞增殖，且呈时间依赖性增加 [6]。
在缺氧性红细胞增多症小鼠模型中，NECA（0.05，0.1µmol/kg；iv；单次注射）显著提高缺氧性红细胞增多症小鼠血清促红细胞生成素水平 [7]。在仅免疫的小鼠中，经鼻给予NECA（50μL；1mM；经鼻给药；单次给药）可显著增加支气管肺泡灌洗液总细胞计数（TCC）、中性粒细胞和嗜酸性粒细胞 [8]。
| Cell experiment [1]: | |
Cell lines | H9c2 cells |
Preparation Method | Cells were washed twice with phosphate-buffered saline (PBS) and then incubated in Tyrode solution for 2h before experiments. To examine the effect of NECA on mitochondrial membrane potential, GSK-3β phosphorylation, and GRP94, cells were exposed to 800μM H2O2 for 20 minutes to cause oxidant damage. A range concentrations of NECA (0.1–10μM) were given 10min before exposing to H2O2. In the study exploring roles of ERS and the cGMP/PKG signaling pathway in NECA-induced cardioprotection against oxidative damage, cells were exposed to 0.1μM NECA/20mM 2-DG/0.1μM KT5823 for 20min. The 2-DG and KT5823 were applied for 10min before the cells were exposed to NECA. |
Reaction Conditions | 0.1–10μM; 20min |
Applications | NECA blocked H2O2-induced GSK-3β phosphorylation and GRP94 expression. |
| Animal experiment [2]: | |
Animal models | Ex-hypoxic polycythemic mice (EHPCM) model |
Preparation Method | This in vivo experiment used the Ex-hypoxic polycythemic mice (EHPCM) model, which induced erythrocytosis by exposing mice to a low-pressure hypoxic environment for a long time. On the 3rd to 6th day after the end of the hypoxic treatment, NECA was given intravenously or intraperitoneally, and finally a short-term hypoxia stimulation was given again. The blood, kidneys and livers of the mice were then collected, and the Epo (erythropoietin) content in the serum and tissues was detected to evaluate the in vivo regulatory effect of NECA on Epo production. |
Dosage form | 0.05, 0.1µmol/kg; iv; single injection |
Applications | NECA significantly increased serum Epo levels in mice with hypoxic erythrocytosis. |
References: | |
| Cas No. | 35920-39-9 | SDF | |
| 别名 | 5'-N-乙基酰胺基腺苷,NECA | ||
| 化学名 | (2S,3S,4R,5S)-5-(6-amino-9H-purin-9-yl)-N-ethyl-3,4-dihydroxytetrahydrofuran-2-carboxamide | ||
| Canonical SMILES | O[C@H]1[C@@H](N2C3=NC=NC(N)=C3N=C2)O[C@H](C(NCC)=O)[C@H]1O | ||
| 分子式 | C12H16N6O4 | 分子量 | 308.3 |
| 溶解度 | ≥ 15.35mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.2436 mL | 16.218 mL | 32.4359 mL |
| 5 mM | 0.6487 mL | 3.2436 mL | 6.4872 mL |
| 10 mM | 0.3244 mL | 1.6218 mL | 3.2436 mL |
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| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
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2.
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- Purity: >99.50%
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