名称 | 5'-N-Ethylcarboxamidoadenosine |
描述 | 5'-N-Ethylcarboxamidoadenosine (NECA) is an agonist of Adenosine receptor, increases cerebral extravasation of fluorescein and low molecular weight dextran independent of blood-brain barrier modulation. |
细胞实验 | A human hepatocellular carcinoma cell line (Hep3B) was employed to determine the in vitro effects of NECA on Epo production and cAMP accumulation. Hep3B cells were carried in a monolayer cell culture and maintained in 75 cm^2 Corning culture flasks containing Eagle's minimal essential medium (MEM) supplemented with 10% fetal bovine serum (PBS), 0.1 m nonessential amino acids, 1 m sodium pyruvate, 100 U/ml penicillin G, and 100 μg/ml streptomycin in a humidified atmosphere of 5% C02/95% air at 37℃. The culture medium was replaced every two days. Cells were detached with trypsin and aliquots of 2.5 x 10^5 viable cells (determined by trypan blue dye exclusion) were transferred to 24 multi-well plates. Each experiment was carried out with low density cells before they reached confluency. The cells were incubated with NECA in concentrations of 1O^9 M to 5 x l0^-5 M in the presence of 1 U/ml adenosine deaminase (ADA) under hypoxic conditions (1% 02, 5% C02, and 94% N2) for 20 hours following 24 hour preincubation in a normoxic atmosphere. At the end of the incubation period, the supernatant was harvested and frozen at -70℃ prior to Epo RIA. The multiple-range test of Duncan was used for the comparison of the several in vitro treatment groups compared with controls[1]. |
体外活性 | 在体外培养的产Epo肝细胞癌(Hep3B)细胞系中,使用5'-N-Ethylcarboxamidoadenosine(≥10(-6)M)处理20小时于低氧条件下(1% O2),与低氧对照组相比,培养基中的Epo水平显著增加。在低氧环境中,以10(-7)M至5 x 10(-5)M浓度范围的5'-N-Ethylcarboxamidoadenosine处理肝细胞癌细胞1小时,其cAMP水平也显著高于低氧对照组。对肝细胞癌细胞膜制备进行的[3H]5'-N-Ethylcarboxamidoadenosine结合的Scatchard分析显示,低亲和力结合位点的解离常数(Kd)为0.44 μM,结合能力为863fM/mg蛋白。这表明,5'-N-Ethylcarboxamidoadenosine在低氧条件下促进Epo产生的增加,至少部分可以归因于刺激与腺苷酸环化酶激活相耦合的腺苷A2受体。 |
体内活性 | 5'-N-Ethylcarboxamidoadenosine,一种腺苷类似物,对红细胞生成素(Epo)的生产有影响。5'-N-Ethylcarboxamidoadenosine(分别为0.05和0.1 mumol/kg i.v.)在缺氧后的多血红蛋白小鼠体内,通过四小时的低氧暴露,显著提高了血清Epo水平(分别为368.8 +/- 56.1和384.6 +/- 45.9 mU/ml),与低氧对照组(133.2 +/- 18.2 mU/ml)相比有显著差异。低氧状态下的肾脏Epo水平为46.4 +/- 13.4 mU/kg肾脏,明显高于常氧肾脏Ep水平(< 1.24 mU/kg肾脏)。茶碱(20 mg/kg i.p.),一种腺苷受体拮抗剂,显著抑制了5'-N-Ethylcarboxamidoadenosine对血清Epo水平的刺激效果[1]。 |
存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
溶解度 | DMSO : 150 mg/mL (486.55 mM)
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关键字 | Adenosine Receptor | Inhibitor | 5'-N-Ethylcarboxamidoadenosine | inhibit | P1 receptor | 5' N Ethylcarboxamidoadenosine | 5'NEthylcarboxamidoadenosine |
相关产品 | Adenosine 5'-monophosphate monohydrate | Inosine | Istradefylline | Adenosine antagonist-1 | Theophylline | Acefylline | Theobromine | Aminophylline | Theophylline monohydrate | Diphylline | FK-453 | Doxofylline |
相关库 | 经典已知活性库 | 已知活性化合物库 | NO PAINS 化合物库 | 抗病毒库 | GPCR靶点分子库 | 膜蛋白靶向化合物库 | 人代谢物化合物库 |