MPP dihydrochloride is a highly selective estrogen receptor alpha (ERα) antagonist. MPP dihydrochloride reduces the ratio of p-ERα/ERα[1].
体外研究 (In Vitro)
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[1]. MPP dihydrochloride shows antiproliferative activity at a concentration of 10 μM in RL95-2 cells[1]. 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[1].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay[1]
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[1]
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[1]
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.
体内研究 (In Vivo)
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)[2].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
Male C57BL/6N mice at the age of 9-10 weeks[2]
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%.
分子量
542.50
Formula
C29H33Cl2N3O3
CAS 号
911295-24-4
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Karaboğa Arslan AK, et al. α-Chaconine and α-Solanine Inhibit RL95-2 Endometrium Cancer Cell Proliferation by Reducing Expression of Akt (Ser473) and ERα (Ser167). Nutrients. 2018 May 25;10(6). pii: E672.
[2]. Labouesse MA, et al. Effects of selective estrogen receptor alpha and beta modulators on prepulse inhibition in male mice. Psychopharmacology (Berl). 2015 Aug;232(16):2981-94.
