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 Aβ plaques in brain tissues from AD patients. tau-0N4R-IN-1 has good pharmacokinetic properties in mice^[1].

tau-0N4R-IN-1 (12.5-100 μM, 2500 min) 抑制了 α-syn 寡聚物的形成, 在 ThT 测定中当浓度为 100 μM 时延迟滞后时间（荧光强度升高的时间），在 PICUP 测定中当浓度为 12.5 至 50 μM 之间发挥抑制作用^[1]。
tau-0N4R-IN-1 (100 μM) 导致 tau 2N3R 和 2N4R （10 μM） 原纤维减少^[1]。
tau-0N4R-IN-1略微降低 tau 0N4R 的寡聚化 (在 100 和 200 μM 剂量下) ^[1]。
tau-0N4R-IN-1 (50 μM, 5 days) 减少从 AD 患者中分离的 Aβ 斑块^[1]。
tau-0N4R-IN-1 (40 μM, 96 h) 防止表达融合蛋白 αS-3K::YFP 的 M17D 神经母细胞瘤细胞中 α-syn 包涵体的形成^[1]。
tau-0N4R-IN-1 (5-20 μM, 48 h) 在 TauRD P301S FRET 生物传感器细胞中具有抗接种作用^[1]。
tau-0N4R-IN-1 (3 μM) 在小鼠微粒体中稳定，在 30 min 时剩余74%^[1]。

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

tau-0N4R-IN-1 (1 mg/kg, 静脉注射，单次) 在 CD1 雄性小鼠体内具有高暴露量和大的血浆分布体积，可透过血脑屏障 (血浆:脑 ≥1)^[1]。

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

285.41

C₁₆H₁₉N₃S

2200453-71-8

Room temperature in continental US; may vary elsewhere.

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

• [1]. Ganegamage, et al. Evaluation of Alpha-Synuclein and Tau Antiaggregation Activity of Urea and Thiourea-Based Small Molecules for Neurodegenerative Disease Therapeutics. ACS chemical neuroscience, 2024, 15(21):3915-3931.  [Content Brief]