1. Neuronal Signaling
  2. Tau Protein α-synuclein Amyloid-β
  3. tau-0N4R-IN-1

tau-0N4R-IN-1 (Compound 6T) is an BBB-penetrable inhibitor of tau 0N4R oligomerization. tau-0N4R-IN-1 effectively inhibits the fibrosis of tau 0N4R, 2N3R, and 2N4R, exhibits an anti-seeding effect on tau in vitro, reduces the oligomerization of α-syn dose-dependently, and prevents formation of α-syn inclusions. tau-0N4R-IN-1 is stable in mouse microsomes and reduces plaques in brain tissues from AD patients. tau-0N4R-IN-1 has good pharmacokinetic properties in mice.

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tau-0N4R-IN-1 Chemical Structure

tau-0N4R-IN-1 Chemical Structure

CAS No. : 2200453-71-8

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Description

tau-0N4R-IN-1 (Compound 6T) is an BBB-penetrable inhibitor of tau 0N4R oligomerization. tau-0N4R-IN-1 effectively inhibits the fibrosis of tau 0N4R, 2N3R, and 2N4R, exhibits an anti-seeding effect on tau in vitro, reduces the oligomerization of α-syn dose-dependently, and prevents formation of α-syn inclusions. tau-0N4R-IN-1 is stable in mouse microsomes and reduces plaques in brain tissues from AD patients. tau-0N4R-IN-1 has good pharmacokinetic properties in mice[1].

In Vitro

tau-0N4R-IN-1 (12.5-100 μM, 2500 min) inhibits the formation of α-syn oligomers with a delayed lag time (time to increase fluorescence intensity) at a concentration of 100 μM in the ThT assay, and between 12.5 and 50 μM in the PICUP assay[1].
tau-0N4R-IN-1 (100 μM) causes a decrease in tau 2N3R and 2N4R (10 μM) protofibrils[1].
tau-0N4R-IN-1 (100 and 200 μM) slightly reduces oligomerization of tau 0N4R[1].
tau-0N4R-IN-1 (50 μM, 5 days) reduces Aβ plaques isolated from AD patients[1].
tau-0N4R-IN-1 (40 μM, 96 h) prevents the formation of α-syn inclusions in M17D neuroblastoma cells expressing the fusion protein αS-3K::YFP [1].
tau-0N4R-IN-1 (5-20 μM, 48 h) has anti-inoculation effects in TauRD P301S FRET biosensor cells[1].
tau-0N4R-IN-1 (3 μM) is stable in mouse microsomes with 74% remaining at 30 min[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

tau-0N4R-IN-1 (1 mg/kg, i.v., single dose) has a high exposure and large plasma volume of distribution, crosses the blood-brain barrier (plasma:brain ratio ≥1) in CD1 male mice[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

285.41

Formula

C16H19N3S

CAS No.
SMILES

S=C(N(C)C1=CC=CC=C1)NC2=CC=C(N(C)C)C=C2

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Please store the product under the recommended conditions in the Certificate of Analysis.

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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tau-0N4R-IN-1
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