BAY 60-6583
目录号 : GC18114
BAY 60-6583是一种高亲和力、高选择性腺苷A2B受体激动剂（EC50 = 2.8nM）。
Cas No.:910487-58-0
Sample solution is provided at 25 µL, 10mM.
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BAY 60-6583 is a high-affinity, highly selective adenosine A2B receptor agonist (EC50 = 2.8nM) [1]. BAY 60-6583 activates the A2B receptor, triggering cAMP signaling and preferential activation of ERK1/2 kinases, thereby exerting anti-inflammatory, antioxidant, and protective effects against cardiac, renal, and cerebral ischemia [2-3]. BAY 60-6583 is primarily used to study ischemia-related injury [4].
In RAW264.7 cells, BAY 60-6583 (0-5μM; 48h) significantly reduced proliferation of cell in a dose-dependent manner [5]. In bone marrow osteoclast, BAY 60-6583 (5μM; 48h) stimulation significantly reduces macrophage colony-stimulating factor-induced osteoclast proliferation [6]. In A549 cells, BAY 60-6583 (1μM; 96h) enhances cell migration and actin remodeling [7].
In MDA-MB-453-luc cells xenograft tumor mouse model, BAY 60-6583 (20μg; iv; 25d) enhances the anti-tumor activity of CAR-T cells [8]. In C57BL6 mice, BAY 60-6583 (100μg/kg; iv; 15min) increases p-Akt and IL-10 levels [9].
References:
[1]. Aherne C M, Saeedi B, Collins C B, et al. Epithelial-specific A2B adenosine receptor signaling protects the colonic epithelial barrier during acute colitis[J]. Mucosal immunology, 2015, 8(6): 1324-1338.
[2]. Bulli I. Adenosine A2B receptors and carbonic anhydrase: new therapeutic targets for cerebral ischemia[J]. 2022.
[3]. Khayat M T, Hanif A, Geldenhuys W J, et al. Adenosine receptors and drug discovery in the cardiovascular system[M]//Frontiers in Cardiovascular Drug Discovery: Volume 4. Bentham Science Publishers, 2019: 16-64.
[4]. Tian Y, Piras B A, Kron I L, et al. Adenosine 2B receptor activation reduces myocardial reperfusion injury by promoting anti‐inflammatory macrophages differentiation via PI3K/Akt pathway[J]. Oxidative medicine and cellular longevity, 2015, 2015(1): 585297.
[5]. Oh Y T, Lee N K. A2b adenosine receptor stimulation down-regulates M-CSF-mediated osteoclast proliferation[J]. Biomedical Science Letters, 2017, 23(3): 194-200.
[6]. Kim H S, Lee N K. The Regulation of p27Kip-1 and Bcl2 Expression Is Involved in the Decrease of Osteoclast Proliferation by A2B Adenosine Receptor Stimulation[J]. Biomedical Science Letters, 2017, 23(4): 327-332.
[7]. Oyama M, Sakamoto M, Kitabatake K, et al. Involvement of cannabinoid receptors and adenosine A2B receptor in enhanced migration of lung cancer A549 cells induced by γ-Ray irradiation[J]. Biological and Pharmaceutical Bulletin, 2024, 47(1): 60-71.
[8]. Tang J, Zou Y, Li L, et al. BAY 60-6583 enhances the antitumor function of chimeric antigen receptor-modified T cells independent of the adenosine A2b receptor[J]. Frontiers in pharmacology, 2021, 12: 619800.
[9]. Ni Y, Liang D, Tian Y, et al. Infarct-sparing effect of adenosine A2B receptor agonist is primarily due to its action on splenic leukocytes via a PI3K/Akt/IL-10 pathway[J]. Journal of Surgical Research, 2018, 232: 442-449.
BAY 60-6583是一种高亲和力、高选择性腺苷A2B受体激动剂（EC50 = 2.8nM） [1]。BAY 60-6583可激活A2B受体，触发cAMP信号传导并优先激活ERK1/2激酶，从而发挥抗炎、抗氧化和保护心脏、肾脏和脑缺血的作用 [2-3]。BAY 60-6583主要用于研究缺血相关损伤 [4]。
在RAW264.7细胞中，BAY 60-6583（0-5μM；48h）以剂量依赖性方式显著降低细胞的增殖 [5]。在骨髓破骨细胞中，BAY 60-6583（5μM；48h）刺激可显著降低巨噬细胞集落刺激因子诱导的破骨细胞增殖 [6]。在A549细胞中，BAY 60-6583（1μM；96h）可增强细胞迁移和肌动蛋白重塑 [7]。
在MDA-MB-453-luc细胞异种移植肿瘤小鼠模型中，BAY 60-6583（20μg/kg；iv；25d）可增强CAR-T细胞的抗肿瘤活性 [8]。在C57BL6小鼠中，BAY 60-6583（100μg/kg；iv；15min）可提高p-Akt和IL-10水平 [9]。
| Cell experiment [1]: | |
Cell lines | RAW264.7 cells |
Preparation Method | After 24 hours of seeding 96-well plates with 2×104 cells/well, the cells were treated with or without BAY 60-6583. BrdU was added 12 hours before culture termination. At the end of the culture period, the cells were fixedwith fixing solution for 30 minutes at room temperature, rinsed twice with phosphate-buffered saline, incubated with monoclonal anti-BrdU antibody for 1 hour followed by antimouse secondary antibody for 30 minutes. After the final wash, substrate was added to the wells followed by stop solution. The proportion of total cells incorporating BrdU into the nucleus was determined by reading the absorbance on a microplate reader at a wavelength of 450nm according to the manufacturer's instructions. |
Reaction Conditions | 0-5μM; 48h |
Applications | BAY 60-6583 significantly reduced proliferation of cell in a dose-dependent manner. |
| Animal experiment [2]: | |
Animal models | MDA-MB-453-luc cells xenograft tumor mouse model |
Preparation Method | Female NOD-PrkdcscidIl2rgnull/Shjh (NPSG) mice (four to eight weeks old) were injected subcutaneously into the right front flank with 3 × 106 MDA-MB-453-luc cells suspended in phenol red-free Matrigel. When the tumors reached a size of 100–150mm3 (1 week after inoculation), 10 × 106 anti-HER2 CAR T cells were intravenously injected into the tumor-bearing mice. After that, mice were intravenously treated with BAY 60-6583 or vehicle control daily (3 mice per group). |
Dosage form | 20μg/kg; iv; 25d |
Applications | BAY 60-6583 enhances the anti-tumor activity of CAR-T cells in xenograft tumor models. |
References: | |
| Cas No. | 910487-58-0 | SDF | |
| 化学名 | 2-((6-amino-3,5-dicyano-4-(4-(cyclopropylmethoxy)phenyl)pyridin-2-yl)thio)acetamide | ||
| Canonical SMILES | O=C(CSC1=NC(N)=C(C#N)C(C2=CC=C(C=C2)OCC3CC3)=C1C#N)N | ||
| 分子式 | C19H17N5O2S | 分子量 | 379.44 |
| 溶解度 | 0.3mg/mL in ethanol, 30mg/mL in DMSO, 25mg/mL in DMF | 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 | 2.6355 mL | 13.1773 mL | 26.3546 mL |
| 5 mM | 0.5271 mL | 2.6355 mL | 5.2709 mL |
| 10 mM | 0.2635 mL | 1.3177 mL | 2.6355 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 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 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
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，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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Quality Control & SDS
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- Purity: >99.50%
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