网站主页 >> CAS数据库列表 >> 4-[3-(2-Chlorophenyl)-2-propen-1-ylidene]-1-phenyl-3,5-pyrazolidinedione
4-[3-(2-Chlorophenyl)-2-propen-1-ylidene]-1-phenyl-3,5-pyrazolidinedione
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- CAS号:
- 310460-39-0
- 英文名:
- 4-[3-(2-Chlorophenyl)-2-propen-1-ylidene]-1-phenyl-3,5-pyrazolidinedione
- 英文别名:
- CPYPP;4-(3-(2-Chlorophenyl)allylidene)-1-phenylpyrazolidine-3,5-dione;4-[3-(2-Chlorophenyl)-2-propen-1-ylidene]-1-phenyl-3,5-pyrazolidinedione;3,5-Pyrazolidinedione, 4-[3-(2-chlorophenyl)-2-propen-1-ylidene]-1-phenyl-;DOCK2,CPYPP,Inhibitor,GEF,Rac1,DOCK180,lymphocytes,autoimmune,DOCK2-Rac1,inhibit,DOCK5,immunosuppressant,migration
- 中文名:
- 4-[3-(2-Chlorophenyl)-2-propen-1-ylidene]-1-phenyl-3,5-pyrazolidinedione
- 中文别名:
- 化合物CPYPP;CPYPP,DOCK2-RAC1相互作用抑制剂;4-(3-(2-氯苯基)亚烯丙基)-1-苯基吡唑烷-3,5-二酮
- CBNumber:
- CB34902763
- 分子式:
- C18H13ClN2O2
- 分子量:
- 324.76
- MOL File:
- 310460-39-0.mol
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4-[3-(2-Chlorophenyl)-2-propen-1-ylidene]-1-phenyl-3,5-pyrazolidinedione化学性质
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密度:
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1.405±0.06 g/cm3(Predicted)
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储存条件:
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2-8°C
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溶解度:
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DMSO: 50 mM
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形态:
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A crystalline solid
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酸度系数(pKa):
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8.26±0.20(Predicted)
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4-[3-(2-Chlorophenyl)-2-propen-1-ylidene]-1-phenyl-3,5-pyrazolidinedione性质、用途与生产工艺
CPYPP 是一种 DOCK2-Rac1 相互作用的抑制剂。CPYPP 结合 DOCK2DHR-2 结构域，并以剂量依赖性方式抑制 DOCK2DHR-2 对 Rac1 的鸟嘌呤核苷酸交换因子活性，IC50 为 22.8 µM。CPYPP 还抑制 DOCK180 和 DOCK5，对 DOCK9 的抑制活性较少。
IC50: 22.8 µM (GEF activity of DOCK2
DHR-2
for Rac1)
CPYPP binds to DOCK2 DHR-2 domain in a reversible manner and inhibited its catalytic activity in vitro. When lymphocytes are treated with CPYPP, both chemokine receptor- and antigen receptor-mediated Rac activation are blocked, resulting in marked reduction of chemotactic response and T cell activation.
Although overexpression of DOCK2 induces Rac activation in HEK293T cells, this activation is markedly suppressed by treating the cells with CPYPP at 100 µM for 1 hr before assay.
When 2.5 mg/kg of CPYPP is administrated intravenously, the plasma concentration of CPYPP is only 2.4 µM at 30 min. However, by intraperitoneally injecting 250 mg/kg of CPYPP into mice, the plasma concentration of CPYPP reached to 11.3 µM at 30 min and 10.9 µM at 1 hr, respectively.
The adoptively transferred spleen cells from mice that has been made by a ‘‘knock-in’’ strategy to express endogenous DOCK2 as a fusion protein with green fluorescent protein (GFP). Intraperitoneal injection of CPYPP (5 mg per mouse) 1 hr before adoptive transfer reduces the percentage of the migrated T cells to <25% of the control level.
4-[3-(2-Chlorophenyl)-2-propen-1-ylidene]-1-phenyl-3,5-pyrazolidinedione
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| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
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| 2024/04/30 | HY-110100 | 4-[3-(2-Chlorophenyl)-2-propen-1-ylidene]-1-phenyl-3,5-pyrazolidinedione
CPYPP | 310460-39-0 | 1mg | 500元 |
| 2024/04/30 | HY-110100 | 4-[3-(2-Chlorophenyl)-2-propen-1-ylidene]-1-phenyl-3,5-pyrazolidinedione
CPYPP | 310460-39-0 | 5mg | 1000元 |
4-[3-(2-Chlorophenyl)-2-propen-1-ylidene]-1-phenyl-3,5-pyrazolidinedione
生产厂家
310460-39-0, 4-[3-(2-Chlorophenyl)-2-propen-1-ylidene]-1-phenyl-3,5-pyrazolidinedione 相关搜索:
- API
- 药靶配体
- CPYPP,DOCK2-RAC1相互作用抑制剂
- 化合物CPYPP
- 4-(3-(2-氯苯基)亚烯丙基)-1-苯基吡唑烷-3,5-二酮
- 310460-39-0
- DOCK2,CPYPP,Inhibitor,GEF,Rac1,DOCK180,lymphocytes,autoimmune,DOCK2-Rac1,inhibit,DOCK5,immunosuppressant,migration
- 4-(3-(2-Chlorophenyl)allylidene)-1-phenylpyrazolidine-3,5-dione
- 3,5-Pyrazolidinedione, 4-[3-(2-chlorophenyl)-2-propen-1-ylidene]-1-phenyl-
- CPYPP
- 4-[3-(2-Chlorophenyl)-2-propen-1-ylidene]-1-phenyl-3,5-pyrazolidinedione