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BAY 60-6583 是一种强效、高亲和力的腺苷 A2B 受体激动剂(EC50 = 3 nM),对A2B 受体的亲和力超过对 A1、A2A 和 A3 受体的亲和力。BAY 60-6583 在心肌缺血模型中具有心脏保护作用。BAY 60-6583 与小鼠、兔子和狗 A2BAR 的结合 Ki 值分别为 750 nM、340 nM 和 330 nM。


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BAY 60-6583 是一种强效、高亲和力的腺苷 A2B 受体激动剂(EC50 = 3 nM),对A2B 受体的亲和力超过对 A1、A2A 和 A3 受体的亲和力。BAY 60-6583 在心肌缺血模型中具有心脏保护作用。BAY 60-6583 与小鼠、兔子和狗 A2BAR 的结合 Ki 值分别为 750 nM、340 nM 和 330 nM。
| 规格 | 价格 | 库存 | 数量 |
|---|---|---|---|
| 1 mg | ¥ 395 | In stock | |
| 5 mg | ¥ 911 | In stock | |
| 10 mg | ¥ 1,160 | In stock | |
| 25 mg | ¥ 2,390 | In stock | |
| 50 mg | ¥ 3,400 | In stock | |
| 100 mg | ¥ 4,770 | In stock | |
| 200 mg | ¥ 6,630 | In stock | |
| 1 mL x 10 mM (in DMSO) | ¥ 977 | In stock |
BAY 60-6583 相关产品
| 产品描述 | BAY 60-6583 is a potent, high-affinity adenosine A2B receptor agonist (EC50 = 3 nM) with affinity for A2B receptors that exceeds that for A1, A2A, and A3 receptors.BAY 60-6583 is cardioprotective in a model of myocardial ischemia.The Ki values for BAY 60-6583 binding to mouse, rabbit, and dog A2BAR were 750 nM, 340 nM, and 330 nM, respectively. The Ki values of BAY 60-6583 binding to A2BAR in mice, rabbits and dogs were 750 nM, 340 nM and 330 nM respectively. |
| 靶点活性 | A2BAR (rabbit):340 nM, A2BAR (dog):330 nM, A2B:3 nM(EC50), A2BAR (mouse):750 nM |
| 体外活性 | BAY 60-6583(0-10 μM)表现出在没有siRNA的情况下,BAY 60-6583的最大激动剂效应为68%。[3] BAY 60-6583(5 μM;24小时)在RAW264.7前破骨细胞内诱导G1期细胞积累的增加,同时减少G2/M期的比例。此外,在相同条件下,BAY 60-6583特异性地抑制了由M-CSF引发的Akt激活,而对M-CSF诱导的ERK1/2激活在RAW264.7前破骨细胞中无明显影响。[4] |
| 体内活性 | BAY 60-6583(100 mg/kg;靜脈注射;兔)在再灌注前給藥,可以減少缺血兔心臟的梗塞面積。[1] BAY 60-6583(2 mg/kg;靜脈注射;小鼠)能夠減輕LPS引起的肺損傷,預先使用此化合物能顯著降低WT小鼠中LPS增加的IL-6水平。[2] |
| 分子量 | 379.44 |
| 分子式 | C19H17N5O2S |
| CAS No. | 910487-58-0 |
| Smiles | NC(=O)CSc1nc(N)c(C#N)c(-c2ccc(OCC3CC3)cc2)c1C#N |
| 密度 | 1.43 g/cm3 (Predicted) |
| 存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| 溶解度信息 | DMSO: 90.0 mg/mL (237.2 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
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