Methylpiperidino pyrazole
Based on 16 publication(s) in Google Scholar
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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- CAS No.: 289726-02-9
- 화학식: C29H31N3O3
- 분자량:469.57
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Methylpiperidino pyrazole
More- Drug Resist Updat. 2023 Nov:71:101014. [Abstract]
- Phytomedicine. 2024 Jan:123:155218. [Abstract]
- Phytomedicine. 2022 May:99:154022. [Abstract]
- J Pharm Anal. 2025 Jul;15(7):101182. [Abstract]
- Ecotoxicol Environ Saf. 2023 Jul 1:259:115060. [Abstract]
- Biochem Pharmacol. 2025 Dec;242(Pt 4):117432. [Abstract]
- Biochem Pharmacol. 2024 Jul:225:116256. [Abstract]
- Cell Biol Toxicol. 2026 Feb 5;42(1):34. [Abstract]
- Biomolecules. 2023 Jul 10;13(7):1097. [Abstract]
- Mol Nutr Food Res. 2021 Sep;65(17):e2100070. [Abstract]
- Metab Brain Dis. 2022 Oct;37(7):2349-2362. [Abstract]
- J Pharm Pharmacol. 2026 Feb 7;78(2):rgag010. [Abstract]
- Brain Res. 2026 Feb 15:1873:150116. [Abstract]
- Biol Reprod. 2025 Jun 15;112(6):1114-1122. [Abstract]
- Food Chem Toxicol. 2023 Jun:176:113792. [Abstract]
- Eur J Inflamm. October 11, 2021.
Biological Activity
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Cell Line
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Type | Value | Description | References |
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| HEC-1 | IC50 |
80 nM
Compound: MPP
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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
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[PMID: 19014882] |
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.
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Cell Line:RL95-2 endometrium cancer cells
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Concentration:1, 5, 10, 25, 50 and 100 µM
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Incubation Time:24 hours
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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.
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Cell Line:RL95-2 cell
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Concentration:10, 15, 20 and 25 µM
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Incubation Time:72 hours
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Result:Showed antiproliferative activity at a concentration of 10 μM.
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Cell Line:RL95-2 cell line
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Concentration:20 µM
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Incubation Time:24 hours
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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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male C57BL/6N mice at the age of 9-10 weeks[2]
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Dosage:Low dose (20 μg/kg body weight) or high dose (200 μg/kg body weight)
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Administration:Administered subcutaneously (s.c.) injected; injection volume of 5 mL/kg; 60 min before PPI testing
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Result:Led to a dose-dependent attenuation of percent PPI. Pretreatment with 200 μg/kg reduced the mean percent PPI scores by ~30%.
Chemical Information
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CAS No. 289726-02-9
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분자량 469.57
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화학식 C29H31N3O3
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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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Synonyms
MPP
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (16)
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Journal Impact Factor
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Most Recent
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Drug Resist Updat
Cisplatin-activated ERβ/DCAF8 positive feedback loop induces chemoresistance in non-small cell lung cancer via PTEN/Akt axis. [Abstract]2023 Nov:71:101014. PMID: 37913652 -
Phytomedicine
Effects and mechanisms of frehmaglutin D and rehmaionoside C improve LPS-induced acute kidney injury through the estrogen receptor-mediated TLR4 pathway in vivo and in vitro. [Abstract]2024 Jan:123:155218. PMID: 37980806 -
Phytomedicine
Silibinin improves L-cell mass and function through an estrogen receptor-mediated antioxidative mechanism. [Abstract]2022 May:99:154022. PMID: 35255283 -
J Pharm Anal
Effect of cholesterol on distribution, cell uptake, and protein corona of lipid microspheres at sites of cardiovascular inflammatory injury. [Abstract]2025 Jul;15(7):101182. PMID: 40735031 -
Ecotoxicol Environ Saf
Bisphenol A interferes with lncRNA Fhadlos2 and RUNX3 association in adolescent mouse ovary. [Abstract]2023 Jul 1:259:115060. PMID: 37229876 -
Biochem Pharmacol
Formononetin alleviates corticosterone-induced myelin damage through activating ERα and promoting the differentiation of oligodendrocyte precursor cells in the prefrontal cortex. [Abstract]2025 Dec;242(Pt 4):117432. PMID: 41110491 -
Biochem Pharmacol
MICAL-L2, as an estrogen-responsive gene, is involved in ER-positive breast cancer cell progression and tamoxifen sensitivity via the AKT/mTOR pathway. [Abstract]2024 Jul:225:116256. PMID: 38729448 -
Cell Biol Toxicol
HUWE1 regulates mitophagy to protect dopaminergic neurons from 6-OHDA- and MPP⁺-induced neurotoxicity. [Abstract]2026 Feb 5;42(1):34. PMID: 41639490 -
Biomolecules
Active Estrogen-Succinate Metabolism Promotes Heme Accumulation and Increases the Proliferative and Invasive Potential of Endometrial Cancer Cells. [Abstract]2023 Jul 10;13(7):1097. PMID: 37509133 -
Mol Nutr Food Res
Diosmetin Protects Against Obesity and Metabolic Dysfunctions Through Activation of Adipose Estrogen Receptors in Mice. [Abstract]2021 Sep;65(17):e2100070. PMID: 34223710 -
Metab Brain Dis
A novel LINC00943/miR-671-5p/ELAVL1 ceRNA crosstalk regulates MPP+ toxicity in SK-N-SH cells. [Abstract]2022 Oct;37(7):2349-2362. PMID: 35779150 -
J Pharm Pharmacol
Formononetin attenuates corticosterone-induced depressive-like behaviors and neuronal damage via ERα/ERK-CREB-BDNF signaling pathway. [Abstract]2026 Feb 7;78(2):rgag010. PMID: 41697882 -
Brain Res
Ezetimibe mitigates microglial activation in Parkinson's disease via TLR4/JNK pathway inhibition: evidence from network pharmacology and experimental validation. [Abstract]2026 Feb 15:1873:150116. PMID: 41419122 -
Biol Reprod
SRA deficiency induces follicular dysplasia by disrupting the hypothalamic Kisspeptin-GPR54 system in mice. [Abstract]2025 Jun 15;112(6):1114-1122. PMID: 40057968 -
Food Chem Toxicol
BPA exposure enhances the metastatic aggression of ovarian cancer through the ERα/AKT/mTOR/HIF-1α signaling axis. [Abstract]2023 Jun:176:113792. PMID: 37080528 -
순도&문서
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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Methylpiperidino pyrazole Related Classifications
HY-127133 Related Classifications
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