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产品总数：61445
| 商品编号 | 规格 | 价格 | 会员价 | 是否有货 | 数量 |
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| PL13304-5mg | 5mg | ¥788.00 | 请登录 |
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| PL13304-10mg | 10mg | ¥1325.00 | 请登录 |
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| PL13304-100mg | 100mg | ¥4955.00 | 请登录 |
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| PL13304-200mg | 200mg | 询价 | 询价 |
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| PL13304-500mg | 500mg | 询价 | 询价 |
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| PL13304-10mM*1mLinDMSO | 10mM*1mLinDMSO | ¥2121.00 | 请登录 |
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| PL13304-1 mL x 10 mM (in DMSO) | ¥743.00 | 请登录 |
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| 中文名称 |
E 2012
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|---|---|
| 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
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| 英文名称 |
E 2012
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| 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
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| Cas No. |
870843-42-8
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| 分子式 |
C25H26FN3O2
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| 分子量 |
419.49
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| 包装储存 |
Powder -20°C 3 years；4°C 2 years
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| 详情描述 |
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。
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| 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。
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|---|---|
| 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.
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| 性状 |
Solid
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| 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.
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| 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.
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| 运输条件 |
Room temperature in continental US; may vary elsewhere.
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| 储存方式 |
Powder -20°C 3 years；4°C 2 years
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| 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.
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| 溶解度数据 |
In Vitro: DMSO : ≥ 50 mg/mL (119.19 mM)配制储备液
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1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。
2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。
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