MPP 二盐酸盐
| 中文名称 | MPP 二盐酸盐 |
|---|---|
| 中文同义词 | MPP 二盐酸盐;化合物 T12101;化合物MPP DIHYDROCHLORIDE (289726-02-9 FREE BASE);4,4'-(4-甲基-5-(4-(2-(哌啶-1-基)乙氧基)苯基)-1H-吡唑-1,3-二基)二苯酚二盐酸盐 |
| 英文名称 | Methyl-piperidino-pyrazole hydrate |
| 英文同义词 | 1,3-Bis(4-hydroxyphenyl)-4-methyl-5-[4-(2-piperidinylethoxy)phenol]-1H-pyrazole dihydrochloride hydrate;MPP dihydrochloride hydrate;Methyl-piperidino-pyrazole hydrate;Methyl-piperidino-pyrazole dihydrochloride hydrate;MPP dihydrochloride (289726-02-9 Free base);MPP dihydrochloride (289726029 Free base),MPP dihydrochloride (289726 02 9 Free base);4,4'-(4-Methyl-5-(4-(2-(piperidin-1-yl)ethoxy)phenyl)-1H-pyrazole-1,3-diyl)diphenol dihydrochloride |
| CAS号 | 911295-24-4 |
| 分子式 | C29H32ClN3O3 |
| 分子量 | 506.04 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 911295-24-4.mol |
| 结构式 |  |
MPP 二盐酸盐 性质
| 储存条件 | Store at -20°C |
|---|---|
| 溶解度 | DMSO：可溶，≥20mg/mL |
| 形态 | 白色粉末 |
MPP dihydrochloride 是一种高度选择性的雌激素受体 α (ERα) 拮抗剂。MPP dihydrochloride 降低了 p-ERα/ERα 的比率。
MPP (1, 5, 10, 25, 50 and 100 µM; 24 h) decreases cell viability with an IC
50
value of 20.01 µM in RL95-2 cells.
MPP dihydrochloride shows antiproliferative activity at a concentration of 10 μM in RL95-2 cells.
MPP dihydrochloride (20 µM; 24 h) reduces the phosphorylation of ERα, while it does not alter the phosphorylation of Akt. MPP dihydrochloride reduces the ratio of p-ERα/ERα.
Cell Viability Assay
| Cell Line: | RL95-2 endometrium cancer cells |
| Concentration: | 1, 5, 10, 25, 50 and 100 µM |
| Incubation Time: | 24 hours |
| Result: | The treatment with 25 µM, 50 µM and 100 µM for 24 h decreased cell viability significantly. However, cell viability was not significantly changed by MPP dihydrochloride at concentration below 25 µM. |
Cell Proliferation Assay
| Cell Line: | RL95-2 cell |
| Concentration: | 10, 15, 20 and 25 µM |
| Incubation Time: | 72 hours |
| Result: | Showed antiproliferative activity at a concentration of 10 μM. |
Western Blot Analysis
| Cell Line: | RL95-2 cell line |
| Concentration: | 20 µM |
| Incubation Time: | 24 hours |
| Result: | Reduced the phosphorylation of ERα, while it did not alter the phosphorylation of Akt. Reduced the ratio of p-ERα/ERα compared to the control group. |
MPP (Low dose 20 μg/kg body weight or high dose 200 μg/kg body weight) leads to a dose-dependent attenuation of percent prepulse inhibition (PPI).
| Animal Model: | Male C57BL/6N mice at the age of 9-10 weeks |
| Dosage: | Low dose (20 μg/kg body weight) or high dose (200 μg/kg body weight) |
| Administration: | Administered subcutaneously (s.c.) injected; injection volume of 5 mL/kg; 60 min before PPI testing |
| Result: | Led to a dose-dependent attenuation of percent PPI. Pretreatment with 200 μg/kg reduced the mean percent PPI scores by ~30%. |