911295-24-4

911295-24-4 structure

Name: MPP dihydrochloride
Chemical Name: 4,4'-(4-Methyl-5-{4-[2-(1-piperidinyl)ethoxy]phenyl}-1H-pyrazole- 1,3-diyl)diphenol dihydrochloride
CAS Number: 911295-24-4
Molecular Formula: C₂₉H₃₃Cl₂N₃O₃
Molecular Weight: 542.497
Catalog: Research Areas Cancer
Create Date: 2017-12-11 07:42:03
Modify Date: 2024-08-30 07:57:17
MPP dihydrochloride is a highly selective estrogen receptor alpha (ERα) antagonist. MPP dihydrochloride reduces the ratio of p-ERα/ERα[1].

Name	4,4'-(4-Methyl-5-{4-[2-(1-piperidinyl)ethoxy]phenyl}-1H-pyrazole- 1,3-diyl)diphenol dihydrochloride
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 Phenol, 4,4'-[4-methyl-5-[4-[2-(1-piperidinyl)ethoxy]phenyl]-1H-pyrazole-1,3-diyl]bis-, hydrochloride (1:2)

Description	MPP dihydrochloride is a highly selective estrogen receptor alpha (ERα) antagonist. MPP dihydrochloride reduces the ratio of p-ERα/ERα[1].
Related Catalog	Signaling Pathways >> Others >> Estrogen Receptor/ERR Research Areas >> Cancer
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	[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. [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.

Molecular Formula	C₂₉H₃₃Cl₂N₃O₃
Molecular Weight	542.497
Exact Mass	541.189880
PSA	70.75000
LogP	7.33250

Hazard Codes	Xi
Risk Phrases	36/37/38
Safety Phrases	26-36

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