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310460-39-0

中文名稱 4-[3-(2-Chlorophenyl)-2-propen-1-ylidene]-1-phenyl-3,5-pyrazolidinedione
英文名稱 4-[3-(2-Chlorophenyl)-2-propen-1-ylidene]-1-phenyl-3,5-pyrazolidinedione
CAS 310460-39-0
分子式 C18H13ClN2O2
分子量 324.76
MOL 文件 310460-39-0.mol
更新日期 2024/12/15 19:35:16
310460-39-0 結(jié)構(gòu)式 310460-39-0 結(jié)構(gòu)式

基本信息

中文別名
化合物CPYPP
4-(3-(2-氯苯基)亞烯丙基)-1-苯基吡唑烷-3,5-二酮
英文別名
CPYPP
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-

物理化學(xué)性質(zhì)

密度1.405±0.06 g/cm3(Predicted)
儲(chǔ)存條件2-8°C
儲(chǔ)存條件Sealed in dry,2-8°C
溶解度DMSO: 50 mM
酸度系數(shù)(pKa)8.26±0.20(Predicted)
形態(tài)結(jié)晶固體
顏色Brown to reddish brown

安全數(shù)據(jù)

危險(xiǎn)性符號(hào)(GHS)GHS hazard pictograms
GHS07
警示詞警告
危險(xiǎn)性描述H302-H315-H319-H335

常見(jiàn)問(wèn)題列表

生物活性
CPYPP 是一種 DOCK2-Rac1 相互作用的抑制劑。CPYPP 結(jié)合 DOCK2DHR-2 結(jié)構(gòu)域,并以劑量依賴性方式抑制 DOCK2DHR-2 對(duì) Rac1 的鳥嘌呤核苷酸交換因子活性,IC50 為 22.8 μM。CPYPP 還抑制 DOCK180 和 DOCK5,對(duì) DOCK9 的抑制活性較少。
靶點(diǎn)

IC50: 22.8 μM (GEF activity of DOCK2 DHR-2 for Rac1)

體外研究

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.

體內(nèi)研究

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.

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156-06-9 538-68-1