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E 2012

CAS No. : 870843-42-8

MCE 站：E 2012

产品活性：E 2012 是有效的 γ 分泌酶调节剂，不会影响 Notch 加工。E 2012 在胆固醇生物合成的*后一步抑制 3β-羟基固醇 Δ24-还原酶 (DHCR24)。E 2012 旨在通过减少淀粉样蛋白 β-42 减少阿兹海默氏病，并在大鼠多次重复给药后诱发白内障。

研究领域：Neuronal Signaling  |  Stem Cell/Wnt

作用靶点：γ-secretase

In Vitro: E2012 has concentration-dependent inhibitory effects on cholesterol biosynthesis in primary culture of rat hepatocytes and HepG2 cells with IC₅₀s of 11.0, and 15.1 nM, respectively.

In Vivo: In vivo lenticular concentration of E 2012 after 13-week repeated dose with cataract was well above those where inhibition is observed in vitro. E 2012 induces cataract in the rat by inhibiting DHCR24 at the final step of cholesterol synthesis with associated elevation in desmosterol within the lens, preceded by desmosterol changes that would serve as a predictive safety biomarker for lenticular opacity.

相关产品：Bioactive Compound Library Plus  |  Neuronal Signaling Compound Library  |  Stem Cell Signaling Compound Library  |  Anti-Aging Compound Library  |  Anti-Alzheimer’s Disease Compound Library  |  DAPT  |  YO-01027  |  LY-411575  |  Compound E  |  L-685458  |  Semagacestat  |  NGP555  |  BMS 299897  |  Sulindac sulfide  |  Begacestat  |  Z-Ile-Leu-aldehyde  |  gamma-secretase modulator 3  |  BMS 433796

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