TTBK1-IN-1 T40348

Product Introduction
Bioactivity


英文名: TTBK1-IN-1

描述: TTBK1-IN-1 is a highly potent and selective inhibitor of tau tubulin kinase 1 (TTBK1), capable of penetrating the blood-brain barrier with ease. With an IC 50 value of 2.7 nM, TTBK1-IN-1 exhibits strong inhibitory activity against TTBK1. This compound holds great promise for advancing research in Alzheimer's disease and other tauopathies.

体外活性: In primary mouse neuronal cultures at DIV14, and analysis of neurite branching is used as a surrogate of neuron health. At acute timepoints (up to 1 h following administration), TTBK1-IN-1 (0.0625-100 μM; 1 hour) has no effect on neurite length when tested up to 100 μM. At chronic effects test, TTBK1-IN-1 (0.0625-100 μM; 6-24 hours) cause a significant decrease in neurite length at the 50 and 100 μM concentrations beginning at 12–18 h following treatment[1].

体内活性: TTBK1-IN-1 (intraperitoneal?injection; 2.5, 7, 20, 60, and 180 mg/kg; 5 min prior to isoflurane treatment) significantly decreases in vivo tau phosphorylation at disease-relevant sites at 180 mg/kg. And there is a trend indicating a dose-responsive effect on tau phosphorylation levels at Ser 422 (20 mg/kg, 21% decrease and 60 mg/kg, 60% decrease, respectively, in tau phosphorylation at Ser 422 vs vehicle-treated control) in isoflurane-induced hypothermia mice model[1].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

关键字: TTBK1 IN 1 | TTBK1IN1 | TTBK-1-IN-1

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