MPP dihydrochloride

Research use only, not for human use.

MPP dihydrochloride is a potent and selective ER (estrogen receptor) modulator. MPP dihydrochloride induces significant apoptosis in the endometrial cancer and oLE cell lines.

MPP dihydrochloride is a potent and selective ER (estrogen receptor) modulator. MPP dihydrochloride induces significant apoptosis in the endometrial cancer and oLE cell lines. MPP dihydrochloride reverses the positive effects of beta-estradiol. MPP dihydrochloride has mixed agonist/antagonist action on murine uterine ERalpha in vivo.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 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 cellsConcentration: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 μMIncubation 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.

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

Estrogen Receptor/ERR

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911295-24-4

542.5

C29H33Cl2N3O3

>98% (HPLC)

DMSO : 30 mg/mL (55.30 mM; Need ultrasonic and warming)

OC1=CC=C(C2=NN(C3=CC=C(O)C=C3)C(C4=CC=C(OCCN5CCCCC5)C=C4)=C2C)C=C1.[H]Cl.[H]Cl

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(-20℃)

With Ice Pack

≥ 2 years