SML2484

AZD3839

≥98% (HPLC)

• 同義詞: (1S)-1-[2-(Difluoromethyl)-4-pyridinyl]-4-fluoro-1-[3-(5-pyrimidinyl)phenyl]-1H-isoindol-3-amine, (S)-1-[2-(Difluoromethyl)pyridin-4-yl]-4-fluoro-1-[3-(pyrimidin-5-yl)phenyl]-1H-isoindol-3-amine, AZD 3839, AZD-3839
• 經驗公式（希爾表示法）: C₂₄H₁₆F₃N₅
• CAS號碼: 1227163-84-9
• 分子量：: 431.41
• MDL號碼: MFCD25976574
• 分類程式碼代碼: 12352200
• NACRES: NA.77

屬性

• 化驗: ≥98% (HPLC)
• 形狀: powder
• 顏色: white to beige
• 溶解度: DMSO: 2 mg/mL, clear
• 儲存溫度: −20°C
• SMILES 字串: NC1=N[C@@](C2=CC=CC(C3=CN=CN=C3)=C2)(C4=CC(C(F)F)=NC=C4)C5=CC=CC(F)=C51

描述

生化／生理作用

AZD3839 is a potent and selective BACE1 inhibitor (Ki = 26.1 nM/BACE1, 372.4 nM/BACE2, >25 μM/Cathepsin D by cell-free TR-FRET; hERG IC50 = 4.8 μM) that effectively suppresses cellular BACE1 activity in neuron cultures (sAPPβ release IC50 = 16.7 nM/SH-SY5Y; Aβ40 release IC50 = 4.8 nM/SH-SY5Y AAP695wt, 32.2 nM/N2A, 24.8 nM/guinea pig cortical neurons, 51 nM/murine cortical neurons) and exhibits in vivo Aβ40-, Aβ42-, sAPPβ-reducing efficacy (80 & 160 μmol/kg mouse, p.o.; 100 & 200 μmol/kg guinea pigs, p.o., 2.5 & 20 μmol/kg cynomolgus monkeys, i.v.) with good pharmacokinetic properties and oral availability.

安全資訊

• 儲存類別代碼: 11 - Combustible Solids
• 水污染物質分類（WGK）: WGK 3
• 閃點（°F）: Not applicable
• 閃點（°C）: Not applicable