| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
ERα ERβ
Estrogen receptor alpha (ERalpha; a mixed agonist/antagonist in vivo). |
|---|---|
| ln Vitro |
In RL95-2 cells, MPP (1, 5, 10, 25, 50, and 100 µM; 24 h) reduces cell viability with an IC50 value of 20.01 µM[1]. At a dose of 10 μM, MPP dihydrochloride has antiproliferative action in RL95-2 cells[1]. MPP dihydrochloride (20 µM; 24 h) decreases ERα phosphorylation but does not change Akt phosphorylation. MPP dihydrochloride lowers the p-ERα/ERα ratio [1].
MPP hydrochloride induces significant apoptosis in endometrial cancer cell lines (e.g., RL95-2) and oLE (ovarian leiomyosarcoma?) cells. It reverses the positive, proliferative effects of beta-estradiol (E2) in these cells. At 10 uM, MPP shows antiproliferative activity in RL95-2 cells. At 20 uM for 24 hours, it reduces the phosphorylation of ERalpha without altering Akt phosphorylation. In vivo, MPP HCl has mixed agonist/antagonist effects on mouse uterine ERalpha. |
| ln Vivo |
Percent prepulse inhibition (PPI) is dose-dependently attenuated by MPP (low dose: 20 μg/kg body weight; high dose: 200 μg/kg body weight)[2].
In vivo, MPP hydrochloride demonstrates mixed agonist and antagonist effects on mouse uterine ERalpha. It can both mimic and block the effects of beta-estradiol depending on the tissue and experimental conditions. The compound is used in mouse models to dissect ERalpha-mediated versus ERbeta-mediated estrogen signaling. However, detailed efficacy data in tumor xenograft models are not widely reported. |
| Enzyme Assay |
Assay: In vitro ERalpha competitive binding assay. Protocol: Recombinant ERalpha ligand-binding domain (LBD) is incubated with varying concentrations of MPP hydrochloride (0.1-1000 nM) and a fluorescently labeled estradiol tracer in a TR-FRET or fluorescence polarization format. Binding affinity (IC50) is determined by measuring displacement of the tracer. Alternatively, radiolabeled 3H-estradiol can be used in a competitive binding assay with scintillation counting.
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: RL95-2 endometrial cancer cells Tested Concentrations: 1, 5, 10, 25, 50 and 100 µM Incubation Duration: 24 hrs (hours) Experimental Results: The treatment with 25 µM, 50 µM and 100 µM for 24 h diminished cell viability Dramatically. However, cell viability was not Dramatically changed by MPP dihydrochloride at concentration below 25 µM. Cell Proliferation Assay[1] Cell Types: RL95-2 endometrium cancer cells Tested Concentrations: 10, 15, 20 and 25 µM Incubation Duration: 72 hrs (hours) Experimental Results: demonstrated antiproliferative activity at a concentration of 10 μM. Western Blot Analysis[1] Cell Types: RL95-2 endometrium cancer cells Tested Concentrations: 20 µM Incubation Duration: 24 hrs (hours) Experimental Results: decreased the phosphorylation of ERα, while it did not alter the phosphorylation of Akt. decreased the ratio of p-ERα/ERα compared to the control group. Cells: Endometrial cancer cell lines (e.g., RL95-2, Ishikawa) and oLE cells. Protocol: Cells are cultured in hormone-depleted (charcoal-stripped) serum to remove endogenous estrogens. Cells are treated with MPP hydrochloride (1-20 uM) alone or in combination with beta-estradiol (1-10 nM) for 24-72 hours. Cell proliferation is measured by MTT or BrdU incorporation assays. Apoptosis is assessed by Annexin V/PI staining and caspase-3/7 activity. ERalpha phosphorylation is analyzed by Western blot using phospho-specific antibodies (e.g., p-Ser118, p-Ser167). |
| Animal Protocol |
Animal/Disease Models: Male C57BL/6N mice at the age of 9-10 weeks[2]
Doses: Low dose (20 μg/kg body weight) or high dose (200 μg/kg body weight) Route of Administration: Administered subcutaneously (sc) (sc) injected; injection volume of 5 mL/kg; 60 min before PPI testing Experimental Results: Led to a dose-dependent attenuation of percent PPI. Pretreatment with 200 μg/kg diminished the mean percent PPI scores by ~30%. Animal Model: Ovariectomized female mice (to eliminate endogenous estrogen). Protocol: Mice are injected subcutaneously with MPP hydrochloride (0.1-10 mg/kg) alone or in combination with beta-estradiol (0.1-1 ug/mouse). The uterine weight is measured after 24-72 hours as a bioassay for estrogenic activity. Additional endpoints include uterine epithelial cell proliferation (by Ki67 immunohistochemistry) and expression of estrogen-responsive genes (e.g., complement C3, lactoferrin) by qRT-PCR. |
| ADME/Pharmacokinetics |
No specific PK data found for MPP hydrochloride; please refer to general properties of selective estrogen receptor modulators (SERMs): SERMs typically exhibit moderate oral bioavailability (20-60%) and long plasma half-lives (12-48 hours) due to extensive enterohepatic recirculation and high plasma protein binding (>95%). Metabolism occurs primarily via CYP3A4, with glucuronidation as a major conjugation pathway.
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| Toxicity/Toxicokinetics |
No specific comprehensive toxicity data found; as an ER modulator, MPP hydrochloride may cause hormone-related side effects including endometrial hyperplasia and thromboembolic events at high doses. However, these are class effects of ER modulation rather than compound-specific toxicities. In ovariectomized mouse models, MPP is generally well-tolerated at doses up to 10 mg/kg. The compound is for research use only and is not intended for human administration.
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| References |
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| Additional Infomation |
MPP hydrochloride is a chemical tool for studying estrogen receptor alpha (ERalpha) signaling. It is particularly valuable for distinguishing ERalpha-mediated from ERbeta-mediated effects due to its selectivity. While it acts as an antagonist in some tissues (e.g., blocking E2-induced proliferation in endometrial cancer cells), it can act as a partial agonist in others (e.g., mouse uterus). It is not FDA-approved for clinical use.
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| Molecular Formula |
C29H32CLN3O3
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|---|---|
| Molecular Weight |
506.03568649292
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| Exact Mass |
505.213
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| CAS # |
2863676-89-3
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| Related CAS # |
MPP dihydrochloride;911295-24-4
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| PubChem CID |
163408961
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
7
|
| Heavy Atom Count |
36
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| Complexity |
621
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| Defined Atom Stereocenter Count |
0
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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.Cl
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| InChi Key |
NUFZYMONJXOTFN-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C29H31N3O3.ClH/c1-21-28(22-5-11-25(33)12-6-22)30-32(24-9-13-26(34)14-10-24)29(21)23-7-15-27(16-8-23)35-20-19-31-17-3-2-4-18-31;/h5-16,33-34H,2-4,17-20H2,1H3;1H
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| Chemical Name |
4-[1-(4-hydroxyphenyl)-4-methyl-5-[4-(2-piperidin-1-ylethoxy)phenyl]pyrazol-3-yl]phenol;hydrochloride
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : 250 mg/mL (494.03 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.11 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.11 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (4.11 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9761 mL | 9.8806 mL | 19.7613 mL | |
| 5 mM | 0.3952 mL | 1.9761 mL | 3.9523 mL | |
| 10 mM | 0.1976 mL | 0.9881 mL | 1.9761 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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