N-[(1S)-1-(氨基羰基)-4 -[(2 - 氯-1-亚氨基乙基氨基]丁基]-苯甲酰胺盐酸盐
N-[(1S)-1-(氨基羰基)-4 -[(2 - 氯-1-亚氨基乙基氨基]丁基]-苯甲酰胺盐酸盐
![N-[(1S)-1-(氨基羰基)-4 -[(2 - 氯-1-亚氨基乙基氨基]丁基]-苯甲酰胺盐酸盐 结构式](https://img.chemicalbook.com/CAS/20180703/GIF/1373232-26-8.gif)
N-[(1S)-1-(氨基羰基)-4 -[(2 - 氯-1-亚氨基乙基氨基]丁基]-苯甲酰胺盐酸盐 性质
| 储存条件 | Store at -20°C |
|---|---|
| 溶解度 | DMF：14mg/mL； DMSO：50mg/mL；乙醇：20mg/mL； PBS（pH 7.2）：3 mg/mL |
| 形态 | 结晶固体 |
| 颜色 | 白色至浅黄色 |
N-[(1S)-1-(氨基羰基)-4 -[(2 - 氯-1-亚氨基乙基氨基]丁基]-苯甲酰胺盐酸盐 用途与合成方法
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 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. |
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. |
N-[(1S)-1-(氨基羰基)-4 -[(2 - 氯-1-亚氨基乙基氨基]丁基]-苯甲酰胺盐酸盐 价格(试剂级)
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024-11-08 | HY-100574A | 1 mg | 502 | ||
| 2024-11-08 | HY-100574A | N-[(1S)-1-(氨基羰基)-4 -[(2 - 氯-1-亚氨基乙基氨基]丁基]-苯甲酰胺盐酸盐 | 1373232-26-8 | 5mg | 1200 |
