6-Hydroxyindole

6-Hydroxyindole is an orally active, endogenous long-acting OATP1B1 inhibitor. 6-Hydroxyindole does not alter the cell surface expression or subcellular localization of OATP1B1. 6-Hydroxyindole protects cells against Ferroptosis. 6-Hydroxyindole possesses intrinsic radical-trapping antioxidant activity. 6-Hydroxyindole serves as a component of oxidative hair dyes. 6-Hydroxyindole can be used in research related to renal failure and neurodegenerative diseases^[1][2][3]. In Vitro:6-Hydroxyindole (0.1-100 μM; 0.5 min-24 h) potently inhibits OATP1B1-mediated substrate uptake in HEK293/OATP1B1 cells via two mechanisms: direct action and long-lasting action, with an IC₅₀ value ranging from 4.52 μM to 43.8 μM^[1].
6-Hydroxyindole (100 μM; 3 h) does not alter the cell surface expression or subcellular localization of OATP1B1 in HEK293/OATP1B1 cells^[1].
6-Hydroxyindole (20 μM; 22-24 h) protects HT-22 mouse hippocampal neurons against Erastin-induced ferroptosis^[2].
6-Hydroxyindole (24 h) inhibits ferroptosis in HT-22 mouse hippocampal neurons, with an EC₅₀ value of 15.8 μM against RSL3 and 8.4 μM against FINO2, and exerts partial protective effects against Erastin-induced ferroptosis^[2].
6-Hydroxyindole (24 h) inhibits ferroptosis in N27 rat dopaminergic neurons, with an EC₅₀ value of 9.1 μM against RSL3 and 8.1 μM against FINO2^[2].
6-Hydroxyindole (0-10³ μM; 7-15 min) exhibits dose-dependent free radical-scavenging antioxidant activity in cell-free ABTS assays^[2].
6-Hydroxyindole (8-5000 μg/plate) exhibits mutagenicity towards *Salmonella typhimurium* strain TA 1535 under both metabolic activation and non-metabolic activation conditions^[3]. In Vivo:6-Hydroxyindole (600 mg/kg; p.o.; single administration) causes death and acute toxicity symptoms in rats. Its maximum tolerated dose is lower than 600 mg/kg, and the LD₅₀ in rats is greater than 600 mg/kg^[3].
6-Hydroxyindole (2000 mg/kg; percutaneous; single administration) does not cause death in rats, with a maximum non-lethal dose greater than 2000 mg/kg^[3].
6-Hydroxyindole (15-240 mg/kg/d; p.o.; daily; gestational days 6-19) causes no maternal toxicity in rats, with only mild fetal ossification retardation observed at high doses^[3].