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TTBK1-IN-1

CAS No. : 2735015-60-6

MCE 国际站：TTBK1-IN-1

产品活性：TTBK1-IN-1 是一种强效、选择性、脑渗透型 tau 微管蛋白激酶 1 (TTBK1) 抑制剂，IC₅₀ 为 2.7 nM。TTBK1-IN-1 可用于阿尔茨海默病及相关疾病的研究。

研究领域：Neuronal Signaling

作用靶点：Tau Protein

In Vitro: 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.

In Vivo: 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.

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