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1373232-26-8

中文名稱 N-[(1S)-1-(氨基羰基)-4 -[(2 - 氯-1-亞氨基乙基氨基]丁基]-苯甲酰胺鹽酸鹽
英文名稱 N-[(1S)-1-(Aminocarbonyl)-4-[(2-chloro-1-iminoethyl)amino]butyl]-benzamide hydrochloride
CAS 1373232-26-8
分子式 C14H20Cl2N4O2
分子量 347.24
MOL 文件 1373232-26-8.mol
更新日期 2024/02/17 22:12:45
1373232-26-8 結構式 1373232-26-8 結構式

基本信息

中文別名
N-[(1S)-1-(氨基羰基)-4 -[(2 - 氯-1-亞氨基乙基氨基]丁基]-苯甲酰胺鹽酸鹽
英文別名
Cl-Amidine (hydrochloride)
N-[(1S)-1-(Aminocarbonyl)-4-[(2-chloro-1-iminoethyl)amino]butyl]-benzamide hydrochloride
Cl-Amidine (hydrochloride) - Sold under license from the University of South Carolina under U.S. Patent No. 7,964,363
所屬類別
有機原料:羧酸類化合物及衍生物

物理化學性質(zhì)

儲存條件-20°C儲存
溶解度DMF: 14 mg/ml; DMSO: 50 mg/ml; Ethanol: 20 mg/ml; PBS (pH 7.2): 3 mg/ml
形態(tài)結晶固體
顏色White to light yellow
N-[(1S)-1-(氨基羰基)-4 -[(2 - 氯-1-亞氨基乙基氨基]丁基]-苯甲酰胺鹽酸鹽價格(試劑級)
報價日期產(chǎn)品編號產(chǎn)品名稱CAS號包裝價格
2026/06/05HY-100574AN-[(1S)-1-(氨基羰基)-4 -[(2 - 氯-1-亞氨基乙基氨基]丁基]-苯甲酰胺鹽酸鹽
Cl-amidine hydrochloride
1373232-26-81 mg502元
2026/06/05HY-100574AN-[(1S)-1-(氨基羰基)-4 -[(2 - 氯-1-亞氨基乙基氨基]丁基]-苯甲酰胺鹽酸鹽
Cl-amidine hydrochloride
1373232-26-85mg1200元
2026/06/05HY-100574AN-[(1S)-1-(氨基羰基)-4 -[(2 - 氯-1-亞氨基乙基氨基]丁基]-苯甲酰胺鹽酸鹽
Cl-amidine hydrochloride
1373232-26-810mM * 1mLin DMSO1320元

常見問題列表

生物活性
Cl-amidine hydrochloride 是口服有效的 PAD 抑制劑,其對 PAD1、PAD3 和 PAD4 的 IC50 值分別為0.8 μM、 6.2 μM 和 5.9 μM。Cl-amidine hydrochloride 可誘導癌細胞的凋亡。Cl-amidine hydrochloride 可誘導 miR-16,引起細胞周期阻滯。Cl-Amidine hydrochloride 可阻斷組蛋白 3 瓜氨酸化和中性粒細胞胞外陷阱的形成,并提高敗血癥小鼠的存活率。
靶點

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

體外研究

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 prevents histone 3 citrullination and neutrophil extracellular trap formation, and improves survival in a murine sepsis model.

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.
體內(nèi)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.
"1373232-26-8" 相關產(chǎn)品信息
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