tc-g 1008

TC-G 1008 (GPR39-C3) is a small molecule, potent, and orally available agonist of G-protein-coupled receptor 39 (GPR39)[4][10][12]. It is widely used in preclinical studies to elucidate the physiological roles of GPR39 activation. TC-G 1008 has demonstrated neuroprotective and anti-inflammatory effects in animal models of hypoxic-ischemic encephalopathy (HIE), reducing brain infarct area and improving both short- and long-term neurological deficits[1]. The drug’s effects are mediated, at least in part, through the SIRT1/PGC-1α/Nrf2 signaling pathway, leading to upregulated expression of anti-inflammatory and antioxidant proteins and downregulated expression of pro-inflammatory cytokines such as IL-6, IL-1β, and TNF-α[1]. Additionally, TC-G 1008 has been shown to promote osteoblast differentiation and mineralization via AMPK activation[6], and has been implicated in anti-depressant-like and anti-anxiety-like responses in mice[3]. However, evidence also suggests that TC-G 1008 may exacerbate seizures and epileptogenesis in certain animal models, acting via both GPR39-dependent and potentially other off-target mechanisms[8]. The compound is selective for GPR39, with minimal binding affinity for other receptors such as ghrelin and neurotensin-1 receptors[4][12].