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ChemicalBook  CAS数据库列表  N-[(1S)-1-(氨基羰基)-4 -[(2 - 氯-1-亚氨基乙基氨基]丁基]-苯甲酰胺

N-[(1S)-1-(氨基羰基)-4 -[(2 - 氯-1-亚氨基乙基氨基]丁基]-苯甲酰胺

生物活性 靶点 体外研究 体内研究
N-[(1S)-1-(氨基羰基)-4 -[(2 - 氯-1-亚氨基乙基氨基]丁基]-苯甲酰胺,913723-61-2,结构式
N-[(1S)-1-(氨基羰基)-4 -[(2 - 氯-1-亚氨基乙基氨基]丁基]-苯甲酰胺
  • CAS号:913723-61-2
  • 英文名:Cl-Amidine
  • 中文名:N-[(1S)-1-(氨基羰基)-4 -[(2 - 氯-1-亚氨基乙基氨基]丁基]-苯甲酰胺
  • CBNumber:CB62590660
  • 分子式:C14H19ClN4O2
  • 分子量:310.78
  • MOL File:913723-61-2.mol
N-[(1S)-1-(氨基羰基)-4 -[(2 - 氯-1-亚氨基乙基氨基]丁基]-苯甲酰胺化学性质
  • 储存条件 :Store at -20°C
  • 溶解度 :Soluble in DMSO

N-[(1S)-1-(氨基羰基)-4 -[(2 - 氯-1-亚氨基乙基氨基]丁基]-苯甲酰胺性质、用途与生产工艺

  • 生物活性 Cl-amidine 是口服有效的 PAD 抑制剂，其对 PAD1、PAD3 和 PAD4 的 IC50 值分别为 0.8 μM、 6.2 μM 和5.9 μM。Cl-amidine 可诱导癌细胞的凋亡。Cl-amidine TFA 可诱导 miR-16，引起细胞周期阻滞。Cl-Amidine 可阻断组蛋白3瓜氨酸化和中性粒细胞胞外陷阱的形成，并提高败血症小鼠的存活率。
  • 靶点

    IC50: 0.8 μM (PAD1), 5.9 μM (PAD4), 6.2 μM (PAD3).

  • 体外研究

    Cl-amidine is a bioavailable haloacetamidine-based compound that inhibits all the active PAD isozymes with near equal potency (k inact /K I =13,000 M -1 •min-1 for PAD4).
    Cl-amidine (0, 5, 10, 15, 20, 25, 50 μg/mL, 24 hours) induces apoptosis in TK6 lymphoblastoid cells and HT29 colon cancer cells in a dose-dependent manner. Interestingly, the colon cancer cell line (HT29) is relatively resistant to apoptosis caused by Cl-amidine.
    Cl-amidine irreversibly inactivates PADs by covalently modifying an active site cysteine that is important for its catalytic activity.

    Apoptosis Analysis.

    Cell Line: TK6 lymphoblastoid cells and HT29 colon cancer cells.
    Concentration: 0, 5, 10, 15, 20, 25, 50 μg/mL.
    Incubation Time: 24 h.
    Result: Induced apoptosis dose-dependently.
  • 体内研究

    Cl-amidine (75 mg/kg, ip once daily) suppresses and treats DSS-induced colitis in mice.
    Cl-amidine (5, 25, 75 mg/kg, oral gavage, once daily) leads to significant reductions in the histology scores dose-dependently.

    Animal Model: C57BL/6 mice (8-12 wk old, DSS mouse model of colitis).
    Dosage: 75 mg/kg.
    Administration: IP once daily.
    Result: Suppressed PAD activity, protein citrullination, and PAD levels in the colon in vivo.
    Animal Model: C57BL/6 mice (8-12 wk old, DSS mouse model of colitis).
    Dosage: 5, 25, 75 mg/kg.
    Administration: Oral gavage once daily.
    Result: Led to significant reductions in the histology scores.
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