BAY 60-6583
目录号 : GC18114
A selective adenosine A2B receptor agonist
Cas No.:910487-58-0
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
BAY 60-6583 is a selective and potent agonist of adenosine A2B receptor with EC50 value of 3 nM [1].
The adenosine A2B receptor is a G-protein coupled adenosine receptor and is activated by high concentrations adenosine. The adenosine A2B receptor plays an important role in anti-inflammatory response and pre/postconditioning cardioprotective [1].
BAY 60-6583 is a potent adenosine A2B receptor agonist. In CHO cells, BAY 60-6583 showed EC50 values of >10000, >10000 and 3 nM respectively for recombinant human A1, A2A and A2B ARs [1]. In BEAS-2B human airway epithelial cells transfected with glucocorticoid response element (GRE) reporter and cAMP-response element (CRE), BAY 60-6583 increased GRE- and CRE-dependent transcription mediated by adenosine A2B receptor that was associated with cAMP formation. Also, BAY 60-6583 increased the expression of CD200, CRISPLD2 and SOCS3, which suppressed the release of proinflammatory mediator [2]. In macrophages derived from arterial injury mice, BAY 60-6583 increased the expression of A2bAR, which then inhibited the released of tumor necrosis factor ɑ (TNF-ɑ) that promoting inflammatory response [3].
In a myocardial ischaemic injury rabbit model, BAY 60-6583 (100 mcg/kg) reduced the infarction area [1].
References:
[1]. Baraldi PG, Tabrizi MA, Fruttarolo F, et al. Recent improvements in the development of A(2B) adenosine receptor agonists. Purinergic Signal, 2008, 4(4): 287-303.
[2]. Greer S, Page CW, Joshi T, et al. Concurrent agonism of adenosine A2B and glucocorticoid receptors in human airway epithelial cells cooperatively induces genes with anti-inflammatory potential: a novel approach to treat chronic obstructive pulmonary disease. J Pharmacol Exp Ther, 2013, 346(3): 473-485.
[3]. Chen H, Yang D, Carroll SH, et al. Activation of the macrophage A2b adenosine receptor regulates tumor necrosis factor-alpha levels following vascular injury. Exp Hematol, 2009, 37(5): 533-538.
| 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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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 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。
3. 以上所有助溶剂都可在 GlpBio 网站选购。