Methylpiperidino pyrazole

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

甲基哌啶基吡唑是一种 ERα 抑制剂，可以阻止 BPS 诱导的 Rb 磷酸化和细胞周期进程。

Methylpiperidino pyrazole is an ERα inhibitor and can prevent the BPS-induced Rb phosphorylation and cell cycle progression.

MPP (1, 5, 10, 25, 50 and 100 μM; 24 h) decreases cell viability with an IC50 value of 20.01 μM in RL95-2 cells.MPP dihydrochloride shows antiproliferative activity at a concentration of 10 μM inRL95-2 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 weeksDosage: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%.

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Endocrinology/Hormones

Estrogen Receptor/ERR

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289726-02-9

469.57

C29H31N3O3

>98% (HPLC)

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Cc1c(-c(cc2)ccc2OCCN2CCCCC2)n(-c(cc2)ccc2O)nc1-c(cc1)ccc1O

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(-20℃)

With Ice Pack

≥ 2 years