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MPP is a highly selective estrogen receptor alpha (ERα) antagonist. MPP reduces the ratio of p-ERα/ERα. https://www.ncbi.nlm.nih.gov/pubmed/29799481 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. https://www.ncbi.nlm.nih.gov/pubmed/25893642

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Methylpiperidino pyrazole Chemical Structure

Methylpiperidino pyrazole Chemical Structure

CAS No. : 289726-02-9

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Description

MPP is a highly selective estrogen receptor alpha (ERα) antagonist. MPP reduces the ratio of p-ERα/ERα[1]. https://www.ncbi.nlm.nih.gov/pubmed/29799481 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. https://www.ncbi.nlm.nih.gov/pubmed/25893642

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].

MedChemExpress (MCE) 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.
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].

MedChemExpress (MCE) 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%.
Molecular Weight

469.57

Formula

C29H31N3O3

CAS No.
SMILES

CC1=C(N(N=C1C2=CC=C(C=C2)O)C3=CC=C(C=C3)O)C4=CC=C(C=C4)OCCN5CCCCC5

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Room temperature in continental US; may vary elsewhere.

Storage

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

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References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Methylpiperidino pyrazole
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