Drug intelligence / Profile preview

bay 60-6583

Development stage
Discontinued
Lead developer
Bayer
Modality
Small Molecules
01

Overview

BAY 60-6583 is a potent and selective small molecule partial agonist of the adenosine A2B receptor (A2BAR), with an EC50 in the low nanomolar range (approximately 2.8–3 nM for murine/human A2B receptors)[2][5][7]. It displays high selectivity for A2B over other adenosine receptor subtypes (A1, A2A, and A3)[5][7]. Mechanistically, it acts as a partial agonist at the adenosine A2B receptor; at high concentrations of endogenous adenosine it may functionally antagonize full agonists[6]. The compound has been widely used as a pharmacological probe in preclinical research to study cardioprotection (e.g., reducing infarct size in myocardial ischemia models), anti-inflammatory effects via cAMP signaling and PI3K/Akt pathway activation, and immunomodulation[1][9]. Developed by Bayer AG as a research tool rather than for clinical use[4], BAY 60‑6583 has shown beneficial effects in animal models of ischemia-reperfusion injury, inflammation-related diseases such as asthma or acute lung injury, urogenital disorders like erectile dysfunction[4], and enhancement of CAR T cell antitumor activity independent of its canonical target[8].

Other names
2-({6-amino-3,5-dicyano-4-[4-(cyclopropylmethoxy)phenyl]pyridin-2-yl}sulfanyl)acetamide
02

Targets

ADORA2B (Adenosine A2B receptor)

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