MedChemExpress - Model C004019 -2417159-57-8

C004019 is a BBB-penatrable and small-molecule PROTAC that targets tau. C004019 can simultaneously recruit tau and E3 ligase, and effectively clear tau proteins by promoting the ubiquitination and proteasome-dependent degradation of tau, thereby improving synaptic and cognitive functions in Alzheimer's disease (AD) mice. C004019 can be used in the research of AD and tau protein-related diseases[1].

C004019

MCE China：C004019

Brand：MedChemExpress (MCE)

Cat. No.HY-138669

CAS：2417159-57-8

Purity：99.37%

Storage：-20°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Shipping：Room temperature in continental US; may vary elsewhere.

Description：C004019 is a BBB-penatrable and small-molecule PROTAC that targets tau. C004019 can simultaneously recruit tau and E3 ligase, and effectively clear tau proteins by promoting the ubiquitination and proteasome-dependent degradation of tau, thereby improving synaptic and cognitive functions in Alzheimer's disease (AD) mice. C004019 can be used in the research of AD and tau protein-related diseases. (Pink: Ligand for target protein (HY-138679); Black: linker (HY-140189); Blue: E3 Ligase Ligand (HY-138678))

In Vitro：C004019 (0.01-100 μM; 24 h) does not cause significant changes in the viability of HEK293 cells stably expressing wild-type full-length human tau (HEK293-hTau)[1]. C004019 (0.01-20 μM; 24 h) inhibits the expression of total tau (Tau5) and phosphorylated tau in HEK293-hTau and SH-SY5Y cells[1].

In Vivo：C004019 (intracerebroventricular injection; 5 μL; 200 μM; single dose) reduces the level of tau protein in the brains of wild-type and 3xTg-AD mice[1]. C004019 (subcutaneous injection; 3-15 mg/kg; single dose) effectively clears tau protein in the brains of wild-type mice[1]. C004019 (subcutaneous injection; 3 mg/kg; once every 6 days for five times) promotes tau clearance and improves cognitive and synaptic functions in hTau and 3xTg-AD mice[1].

References：

[1]. Wang W, et al. A novel small-molecule PROTAC selectively promotes tau clearance to improve cognitive functions in Alzheimer-like models. Theranostics. 2021 Mar 11;11(11):5279-5295. [Content Brief]

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MedChemExpress - Model C004019 -2417159-57-8

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C004019