BAY 60-6583

A selective adenosine A2B receptor agonist

此产品仅用于科学研究，我们不为任何个人用途提供产品和服务

库存: 现货

可选规格

包装

价格

促销价

数量
1mg

￥312.00

250.00

- +
5mg

￥1212.00

970.00

- +
10mg

￥1525.00

1220.00

- +
25mg

￥3575.00

2860.00

- +

已选 0 种 0 瓶

金额: ￥0.00

首页收藏

货号: ajci20470
CAS: 910487-58-0
别名:
分子式: C19H17N5O2S
分子量: 379.44
纯度: >98%
溶解度: 0.3mg/mL in ethanol, 30mg/mL in DMSO, 25mg/mL in DMF
储存: Store at -20°C
库存: 现货

Background

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].

参考文献:
[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.