4-[3-(2-Chlorophenyl)-2-propen-1-ylidene]-1-phenyl-3,5-pyrazolidinedione
中文名称 | 4-[3-(2-Chlorophenyl)-2-propen-1-ylidene]-1-phenyl-3,5-pyrazolidinedione |
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中文同义词 | 4-(3-(2-氯苯基)亚烯丙基)-1-苯基吡唑烷-3,5-二酮;化合物CPYPP;CPYPP,DOCK2-RAC1相互作用抑制剂 |
英文名称 | 4-[3-(2-Chlorophenyl)-2-propen-1-ylidene]-1-phenyl-3,5-pyrazolidinedione |
英文同义词 | 4-[3-(2-Chlorophenyl)-2-propen-1-ylidene]-1-phenyl-3,5-pyrazolidinedione;CPYPP;3,5-Pyrazolidinedione, 4-[3-(2-chlorophenyl)-2-propen-1-ylidene]-1-phenyl-;4-(3-(2-Chlorophenyl)allylidene)-1-phenylpyrazolidine-3,5-dione;DOCK2,CPYPP,Inhibitor,GEF,Rac1,DOCK180,lymphocytes,autoimmune,DOCK2-Rac1,inhibit,DOCK5,immunosuppressant,migration |
CAS号 | 310460-39-0 |
分子式 | C18H13ClN2O2 |
分子量 | 324.76 |
EINECS号 | |
相关类别 | API |
Mol文件 | 310460-39-0.mol |
结构式 | ![]() |
4-[3-(2-Chlorophenyl)-2-propen-1-ylidene]-1-phenyl-3,5-pyrazolidinedione 性质
密度 | 1.405±0.06 g/cm3(Predicted) |
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储存条件 | 2-8°C |
溶解度 | 二甲基亚砜:50 mM |
形态 | 结晶固体 |
酸度系数(pKa) | 8.26±0.20(Predicted) |
颜色 | 棕至红棕色 |
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.
安全信息
更新日期 | 产品编号 | 产品名称 | CAS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 |