2. Vitamin D Related/Nuclear Receptor
  3. Estrogen Receptor/ERR
  4. Methylpiperidino pyrazole

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

Methylpiperidino pyrazole Chemical Structure

CAS No. : 289726-02-9

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Methylpiperidino pyrazole Related Antibodies

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Description

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[1][2][3].

Cellular Effect
Cell Line Type Value Description References
HEC-1 IC50
80 1
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]
HEC-1 IC50
80 1
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]
HEC-1 IC50
80 1
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.

Methylpiperidino pyrazole Related Antibodies

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%.
Masse moléculaire

469.57

Formule

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
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
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Methylpiperidino pyrazole Related Classifications

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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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