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MPP dihydrochloride 

目录号: HY-103454
产品使用指南

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。

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MPP dihydrochloride Chemical Structure

MPP dihydrochloride Chemical Structure

CAS No. : 911295-24-4

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Description

MPP dihydrochloride is a highly selective estrogen receptor alpha (ERα) antagonist. MPP dihydrochloride reduces the ratio of p-ERα/ERα[1].

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].

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.
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].

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%.
Molecular Weight

542.50

Formula

C₂₉H₃₃Cl₂N₃O₃

CAS No.

911295-24-4

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
  • 摩尔计算器

  • 稀释计算器

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This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

MPPEstrogen Receptor/ERRAktERαRL95-2endometriumcancerInhibitorinhibitorinhibit

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产品名称:
MPP dihydrochloride
目录号:
HY-103454
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