Mirabegron is a potent (EC50 = 22.4 nM CHO cells expressing human ß3-ARs) beta-3 adrenergic receptor (ß3-AR) agonist with high selectivity over the beta-1 and beta-2 receptors.1 Clinically useful for the treatment of overactive bladder syndrome. Chronic treatment of human subjects with mirabegron increased brown adipose tissue (BAT) metabolic activity, increased HDL and bile acid levels, and produced substantial improvements in glucose and insulin metabolism.2 Mirabegron inhibited tumor growth in various tumor models including pancreatic ductal adenocarcinoma and hepatocellular carcinoma via altering global metabolism in an uncoupling protein 1 (UCP1, a key protein for non-shivering thermogenesis) dependent manner.3
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