TTBK1-IN-1 is a potent, selective and brain-penetranttau tubulin kinase 1 (TTBK1)inhibitor with anIC₅₀of 2.7 nM. TTBK1-IN-1 can be used for the research of alzheimer’s disease and related tauopathies^[1].

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].

TTBK1-IN-1 (intraperitoneal injection; 2.5, 7, 20, 60, and 180 mg/kg; 5 min prior to isoflurane treatment) significantly decreasesin vivotau 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].

337.38

C₁₈H₁₉N₅O₂

2735015-60-6

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