GIV3727

GIV3727 is an orally active bitter taste receptor antagonist targeting TAS2R4, TAS2R7, TAS2R20, TAS2R31, TAS2R40, and TAS2R43, with orthosteric, insurmountable antagonism at hTAS2R31. GIV3727 blocks TAS2R4 and prevents Gallic acid-induced upregulation of GDF15 mRNA expression. GIV3727 inhibits agonist-evoked receptor activation. GIV3727 reduces the perceived bitterness of acesulfame K and saccharin without affecting sweet taste perception. GIV3727 can be used for obesity research^[1][2]. In Vitro:The TAS2R antagonist GIV3727 (110 µM; 30 min) blocks gallic acid-induced GDF15 mRNA expression in primary jejunal crypts but does not affect GLP-1 mRNA expression or azithromycin-induced GDF15 mRNA expression^[1].
GIV3727 (6.4 μM; acesulfame K) is a novel, reversible antagonist of hTAS2R31, inhibiting activation by acesulfame K and saccharin with IC₅₀ values of 6.4 μM and 7.9 μM, respectively, and also inhibits hTAS2R43^[2].
GIV3727 (6-25 μM) acts as an orthosteric, insurmountable antagonist of hTAS2R31, increasing agonist EC₅₀ 3- to 10-fold and decreasing maximal signal amplitude by 35-70% at 25 μM^[2].
GIV3727 (6-25 μM) significantly reduces hTAS2R31 receptor activation across all concentrations of acesulfame K, saccharin, and aristolochic acid^[2].