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

Methylpiperidino pyrazole  (Synonyms: MPP)

目录号: HY-127133
产品使用指南 技术支持

Methylpiperidino pyrazole (MPP) 是一种强效的选择性 ER (雌激素受体)调节剂。Methylpiperidino pyrazole 可诱导子宫内膜癌和 oLE 细胞凋亡。Methylpiperidino pyrazole 可逆转 β - 雌激素的积极作用。在体内，Methylpiperidino pyrazole 对小鼠子宫 ERalpha 具有激动剂和拮抗剂的混合作用。

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Methylpiperidino pyrazole Chemical Structure

Methylpiperidino pyrazole Chemical Structure

CAS No. : 289726-02-9

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Methylpiperidino pyrazole 的其他形式现货产品:

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Methylpiperidino pyrazole 相关抗体

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Estrogen receptor ERα ERβ ERRα ERRβ ERRγ

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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].

细胞效力
(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]
体外研究
(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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Methylpiperidino pyrazole 相关抗体:

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.
体内研究
(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].

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%.
分子量

469.57

Formula

C29H31N3O3
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

Methylpiperidino pyrazole 相关分类

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  • 稀释计算器

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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× = ×
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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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