BAY 60-6583

Short Summary : Potent A2B receptor agonist

Category : GPCR/G protein|Adenosine Receptor

Purity : 0.98

CAS Number : 910487-58-0

Formula : C19H17N5O2S

Molecular Weight :

Molecular Weight : 379.44

SMILE : O=C(CSC1=NC(N)=C(C#N)C(C2=CC=C(C=C2)OCC3CC3)=C1C#N)N

Solubility : Soluble in DMSO > 10 mM

Storage : Store at -20°C

Description : 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 (TNF-) 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.

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