Denatonium (benzoate)

Denatonium benzoate (THS-839) is known as the most bitter compound and is commonly used as a deterrent (bittering agent) to activate different types of bitter taste receptors (TAS2Rs) with oral activity. Denatonium benzoate can enhance insulin secretion, has anti-inflammatory effects, and promotes allergy susceptibility^{[1] [2] [3][4]}. IC50 & Target:TAS2Rs In Vitro:Denatonium benzoate (15 μM, 5 min) reduces the spontaneous contraction activity of rat gastric smooth muscle strips^[1].
Denatonium benzoate (10 μM, 24h) increases the release of β-hexosaminidase and the mobilization of Ca²⁺ in IgE-mediated activated RBL-2H3 and KU812 cells^[2].
Denatonium benzoate (10 μM, 30 min) enhances the expression of FcεRIα on the surface of RBL-2H3 and KU812 cells^[2].
Denatonium benzoate (0-25 mM, 24 h) inhibits the proliferation of RBL-2H3 and KU812 cells when above 0.1 mM^[2]. In Vivo:Denatonium benzoate (15mg/kg, intraperitoneal injection, single dose) can reduce the initial stage of foot inflammation in rats induced by histamine^[1].
Denatonium benzoate (5 mg/kg, i.g., single dose) promotes allergy susceptibility in mice^[2].