289726-02-9
289726-02-9 structure
- Name: Methylpiperidino pyrazole
- Chemical Name: 4-[2-(4-hydroxyphenyl)-4-methyl-3-[4-(2-piperidin-1-ylethoxy)phenyl]-1H-pyrazol-5-ylidene]cyclohexa-2,5-dien-1-one,dihydrochloride
- CAS Number: 289726-02-9
- Molecular Formula: C29H31N3O3
- Molecular Weight: 469.57
- Create Date: 2016-02-12 15:07:30
- Modify Date: 2024-01-01 23:50:19
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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/29799481Labouesse 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
| Name | 4-[2-(4-hydroxyphenyl)-4-methyl-3-[4-(2-piperidin-1-ylethoxy)phenyl]-1H-pyrazol-5-ylidene]cyclohexa-2,5-dien-1-one,dihydrochloride |
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| Synonyms |
4,4'-(4-Methyl-5-{4-[2-(piperidin-1-yl)ethoxy]phenyl}-1H-pyrazole-1,3-diyl)diphenol dihydrochloride
4,4'-(4-Methyl-5-{4-[2-(1-piperidinyl)ethoxy]phenyl}-1H-pyrazole-1,3-diyl)diphenol dihydrochloride MPP dihydrochloride hydrate Phenol, 4,4'-[4-methyl-5-[4-[2-(1-piperidinyl)ethoxy]phenyl]-1H-pyrazole-1,3-diyl]bis-, hydrochloride (1:2) MPP dihydrochloride Methyl-piperidino-pyrazole hydrate |
| 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/29799481Labouesse 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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| 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%. |
| References |
| Molecular Formula | C29H31N3O3 |
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| Molecular Weight | 469.57 |
| Exact Mass | 541.189880 |
| PSA | 70.75000 |
| LogP | 7.33250 |
| Hazard Codes | Xi |
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