870843-42-8
中文名稱
(E)-1-[(1S)-1-(4-氟苯基)乙基]-3-[3-甲氧基-4-(4-甲基-1H-咪唑-1-YL)亞芐基]哌啶-2-酮
英文名稱
(E)-1-[(1S)-1-(4-Fluorophenyl)ethyl]-3-[3-methoxy-4-(4-methyl-1H-imidazol-1-yl)benzylidene]piperidin-2-one
CAS
870843-42-8
分子式
C25H26FN3O2
分子量
419.49
MOL 文件
870843-42-8.mol
870843-42-8 結(jié)構(gòu)式
基本信息
中文別名
(E)-1-[(1S)-1-(4-氟苯基)乙基]-3-[3-甲氧基-4-(4-甲基-1H-咪唑-1-基)亞芐基]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)亞芐基]哌啶-2-酮
英文別名
E 2012CS-510
E-2012
E2012
E2012
E 2012
E-2012
1-[(1S)-1-(4-fluorophenyl)ethyl]-3-[[3-Methoxy-4-(4-Methyl-1H-iMidazol-1-yl)phenyl]Methylene]-
(E)-1-[(1S)-1-(4-Fluorophenyl)ethyl]-3-[3-methoxy-4-(4-methyl-1H-imidazol-1-yl)benzylidene]pip
(E)-1-[(1S)-1-(4-Fluorophenyl)ethyl]-3-[3-methoxy-4-(4-methyl-1H-imidazol-1-yl)benzylidene]piperi
(S,E)-1-(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
(E)-1-[(IS)-1-(4-fluorophenyl)ethyl]-3-[3-methoxy-4-(4-methyl-1H-imidazol-1 -y1) benzylidene]piperidin-2-one
所屬類別
生物化工：激動(dòng)劑抑制劑物理化學(xué)性質(zhì)
沸點(diǎn)649.2±55.0 °C(Predicted)
密度1.19±0.1 g/cm3(Predicted)
儲(chǔ)存條件-20°C儲(chǔ)存
溶解度DMF: 10mg/mL; DMSO: 10mg/mL; DMSO:PBS (pH 7.2) (1:3): 0.25mg/mL; Ethanol: 10mg/mL
酸度系數(shù)(pKa)5.67±0.61(Predicted)
形態(tài)粉末
顏色Light yellow to yellow
(E)-1-[(1S)-1-(4-氟苯基)乙基]-3-[3-甲氧基-4-(4-甲基-1H-咪唑-1-YL)亞芐基]哌啶-2-酮價(jià)格(試劑級(jí))
| 報(bào)價(jià)日期 | 產(chǎn)品編號(hào) | 產(chǎn)品名稱 | CAS號(hào) | 包裝 | 價(jià)格 |
| 2024/11/08 | HY-10016 | (E)-1-[(1S)-1-(4-氟苯基)乙基]-3-[3-甲氧基-4-(4-甲基-1H-咪唑-1-YL)亞芐基]哌啶-2-酮 E 2012 | 870843-42-8 | 5mg | 1200元 |
| 2024/11/08 | HY-10016 | (E)-1-[(1S)-1-(4-氟苯基)乙基]-3-[3-甲氧基-4-(4-甲基-1H-咪唑-1-YL)亞芐基]哌啶-2-酮 E 2012 | 870843-42-8 | 10mM * 1mLin DMSO | 1320元 |
| 2024/11/08 | HY-10016 | (E)-1-[(1S)-1-(4-氟苯基)乙基]-3-[3-甲氧基-4-(4-甲基-1H-咪唑-1-YL)亞芐基]哌啶-2-酮 E 2012 | 870843-42-8 | 10mg | 1800元 |
常見(jiàn)問(wèn)題列表
生物活性
E 2012 是有效的 γ 分泌酶調(diào)節(jié)劑，不會(huì)影響 Notch 加工。E 2012 在膽固醇生物合成的最后一步抑制 3β-羥基固醇 Δ24-還原酶 (DHCR24)。E 2012 旨在通過(guò)減少淀粉樣蛋白 β-42 減少阿茲海默氏病，并在大鼠多次重復(fù)給藥后誘發(fā)白內(nèi)障。體外研究
E2012 has concentration-dependent inhibitory effects on cholesterol biosynthesis in primary culture of rat hepatocytes and HepG2 cells with IC 50 s of 11.0, and 15.1 nM, respectively.
體內(nèi)研究
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.