网站主页 >> 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
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- CAS号:
- 913723-61-2
- 英文名:
- Cl-Amidine
- 英文别名:
- Cl-Amidine;N-BCl-I-OA cpd;Cl amidine,Clamidine;N-alpha-Benzoyl-N5-(2-chloro-1-iminoethyl)-1-ornithine amide;N-[(1S)-1-(Aminocarbonyl)-4-[(2-chloro-1-iminoethyl)amino]butyl]benzamide;Benzamide, N-[(1S)-1-(aminocarbonyl)-4-[(2-chloro-1-iminoethyl)amino]butyl]-;N-[(1S)-1-(Aminocarbonyl)-4-[(2-chloro-1-iminoethyl)amino]butyl]-benzamideN-
- 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
- 中文别名:
- 化合物 T10831;N-ALPHA-苯甲酰基-N5-(2-氯-1-亚氨基乙基)-1-鸟氨酰胺;N-[(1S)-1-(氨基羰基)-4 -[(2 - 氯-1-亚氨基乙基氨基]丁基]-苯甲酰胺
- CBNumber:
- CB62590660
- 分子式:
- C14H19ClN4O2
- 分子量:
- 310.78
- MOL File:
- 913723-61-2.mol
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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
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储存条件:
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Store at -20°C
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溶解度:
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Soluble in DMSO
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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
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。
IC50: 0.8 μM (PAD1), 5.9 μM (PAD4), 6.2 μM (PAD3).
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.
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Cell Line:
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TK6 lymphoblastoid cells and HT29 colon cancer cells.
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Concentration:
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0, 5, 10, 15, 20, 25, 50 μg/mL.
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Incubation Time:
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24 h.
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Result:
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Induced apoptosis dose-dependently.
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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.
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Animal Model:
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C57BL/6 mice (8-12 wk old, DSS mouse model of colitis).
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Dosage:
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75 mg/kg.
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Administration:
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IP once daily.
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Result:
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Suppressed PAD activity, protein citrullination, and PAD levels in the colon in vivo.
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Animal Model:
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C57BL/6 mice (8-12 wk old, DSS mouse model of colitis).
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Dosage:
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5, 25, 75 mg/kg.
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Administration:
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Oral gavage once daily.
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Result:
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Led to significant reductions in the histology scores.
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N-[(1S)-1-(氨基羰基)-4 -[(2 - 氯-1-亚氨基乙基氨基]丁基]-苯甲酰胺
上下游产品信息
上游原料
下游产品
N-[(1S)-1-(氨基羰基)-4 -[(2 - 氯-1-亚氨基乙基氨基]丁基]-苯甲酰胺
生产厂家
913723-61-2, N-[(1S)-1-(氨基羰基)-4 -[(2 - 氯-1-亚氨基乙基氨基]丁基]-苯甲酰胺 相关搜索:
- 化合物 T10831
- N-ALPHA-苯甲酰基-N5-(2-氯-1-亚氨基乙基)-1-鸟氨酰胺
- N-[(1S)-1-(氨基羰基)-4 -[(2 - 氯-1-亚氨基乙基氨基]丁基]-苯甲酰胺
- 913723-61-2
- N-BCl-I-OA cpd
- Cl amidine,Clamidine
- Benzamide, N-[(1S)-1-(aminocarbonyl)-4-[(2-chloro-1-iminoethyl)amino]butyl]-
- N-alpha-Benzoyl-N5-(2-chloro-1-iminoethyl)-1-ornithine amide
- N-[(1S)-1-(Aminocarbonyl)-4-[(2-chloro-1-iminoethyl)amino]butyl]benzamide
- N-[(1S)-1-(Aminocarbonyl)-4-[(2-chloro-1-iminoethyl)amino]butyl]-benzamideN-
- Cl-Amidine