Methylpiperidino pyrazole (Synonyms: MPP)

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

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Methylpiperidino pyrazole Chemical Structure

CAS No. : 289726-02-9

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Other Forms of Methylpiperidino pyrazole:

MPP dihydrochloride Get quote
MPP hydrochloride Get quote

8 Publications Citing Use of MCE Methylpiperidino pyrazole

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Estrogen receptor ERα ERβ ERRα ERRβ ERRγ

Biological Activity
Purity & Documentation
References
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Description

Cellular Effect

Cell Line	Type	Value	Description	References
HEC-1	IC₅₀	80 nM Compound: MPP	Antagonist activity at human ERalpha receptor expressed in HEC1 cells assessed as transcriptional activation after 24 hrs by luciferase reporter gene assay Antagonist activity at human ERalpha receptor expressed in HEC1 cells assessed as transcriptional activation after 24 hrs by luciferase reporter gene assay	[PMID: 19014882]

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.

289726-02-9

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation

Handling Instructions (2659 KB)

References

[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. [Content Brief]

[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. [Content Brief]

[3]. Davis AM, et al. The effects of the selective estrogen receptor modulators, methyl-piperidino-pyrazole (MPP), and raloxifene in normal and cancerous endometrial cell lines and in the murine uterus. Mol Reprod Dev. 2006 Aug;73(8):1034-44. [Content Brief]

Methylpiperidino pyrazole Related Classifications

Endocrinology

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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.

Keywords:

Methylpiperidino pyrazole289726-02-9MPPEstrogen Receptor/ERRAktERαRL95-2endometriumcancerInhibitorinhibitorinhibit

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