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Description: GSK3179106 is a novel, potent, selective, and gut-restricted RET kinase inhibitor with an IC50 of 0.4 nM. In all the rat models, RET inhibition with GSK3179106 attenuated the number of abdominal contractions induced by CRD. Our findings identify a role for RET in visceral nociception. Inhibition of RET kinase with a potent, selective, and gut-restricted small molecule may represent a novel therapeutic strategy for the treatment of IBS through the attenuation of post-inflammatory and stress-induced visceral hypersensitivity.
References: Neurogastroenterol Motil. 2018 Oct 12:e13479.; J Pharmacol Exp Ther. 2019 Feb; 368(2):299-307.
Related CAS#:1884420-19-2 (GSK3179106 hydrate)
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