E 2012|870843-42-8|-陌孚医药/Medlife

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E 2012

目录号: PL13304 纯度: ≥97%

CAS No. :870843-42-8

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中文名称	E 2012
中文别名	(E)-1-[(1S)-1-(4-氟苯基)乙基]-3-[3-甲氧基-4-(4-甲基-1H-咪唑-1-基)亚苄基]哌啶-2-酮;(E)-1-[(1S)-1-(4-氟苯基)乙基]-3-[3-甲氧基-4-(4-甲基-1H-咪唑-1-yl)亚苄基]哌啶-2-酮
英文名称	E 2012
英文别名	(E)-1-[(1S)-1-(4-Fluorophenyl)ethyl]-3-[3-methoxy-4-(4-methyl-1H-imidazol-1-yl)benzylidene]piperidin-2-one;(3E)-1-[(1S)-1-(4-fluorophenyl)ethyl]-3-[[3-methoxy-4-(4-methylimidazol-1-yl)phenyl]methylidene]piperidin-2-one;E 2012;(3E)-1-[(1S)-1-(4-fluorophenyl)ethyl]-3-[3-methoxy-4-(4-methyl-1H-imidazol-1-yl)benzylidene]piperidin-2-one;(e)-1-((1s)-1-(4-fluorophenyl)ethyl)-3-(3-methoxy-4-(4-methyl-1h-imidazol-1-yl)benzylidene)piperidin-2-one;(S,E)-1-(1-(4-fluorophenyl)ethyl)-3-(3-methoxy-4-(4-methyl-1H-imidazol-1-yl)benzylidene)piperidin-2-one;E-2012;3LSD4Y5F0F;E2012;PUOAETJYKQITMO-LANLRWRYSA-N;(3E)-1-[(1S)-1-(4-fluorophenyl)ethyl]-3-[3-methoxy-4-(4-methyl-1
Cas No.	870843-42-8
分子式	C₂₅H₂₆FN₃O₂
分子量	419.49
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情	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最后一步抑制 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。
生物活性	E 2012 is a potent gamma (γ) secretase modulator without affecting Notch processing. E 2012 inhibits 3β-hydroxysterol Δ24-reductase (DHCR24) at the final step in the cholesterol biosynthesis. E 2012 aims at Alzheimers disease by reduction of amyloid β-42, and induces cataract following repeated doses in the rat.
性状	Solid
体外研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Powder -20°C 3 years；4°C 2 years
参考文献	[1]. Nakano-Ito K, et al. E2012-induced cataract and its predictive biomarkers. Toxicol Sci. 2014 Jan;137(1):249-58. [2]. Portelius E, Van Broeck B, Andreasson U, Gustavsson MK, Mercken M, Zetterberg H, Borghys H, Blennow K.Acute effect on the Aβ isoform pattern in CSF in response to γ-secretase modulator and inhibitor treatment in dogs.J Alzheimers Dis. 2010;21(3):1005-12.

溶解度数据	In Vitro: DMSO : ≥ 50 mg/mL (119.19 mM)配制储备液

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