| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Targets |
MPP dihydrochloride specifically targets estrogen receptor alpha (ERalpha) with high affinity, displaying over 200-fold selectivity for ERalpha over ERbeta. It binds to the ligand-binding domain of ERalpha, acting as a silent antagonist that prevents receptor activation and subsequent transcriptional activity. The compound does not exhibit any detectable agonist activity at physiological concentrations.
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| ln Vitro |
MPP dihydrochloride (1, 5, 10, 25, 50, and 100 μM; 24 hours) has an IC50 value of 20.01 μM, which lowers the viability of RL95-2 cells [1]. 10 μM of MPP dihydrochloride in RL95-2 MPP dihydrochloride (20 μM; 24 h) decreases phosphorylation of ERα but does not change phosphorylation of Akt. The phosphorylation of p-ERα/ERα is decreased by MPP dihydrochloride [1]. demonstrates anti-proliferative properties in cells [1].
In primary hippocampal cells, MPP dihydrochloride at concentrations ranging from 1 pM to 1 microM has been studied for its effects on neuroprotection. It is used to block ERalpha-dependent pathways in cell survival assays. When used alone or in combination with other compounds, it helps dissect the relative contributions of ERalpha versus ERbeta in various cellular processes, including oxidative stress protection and cell survival. |
| ln Vivo |
Prepulse index (PPI) is attenuated in a dose-dependent manner by MPP dihydrochloride (20 μg/kg or 200 μg/kg) [2].
No specific in vivo activity data is available for MPP dihydrochloride alone. In animal studies, it is typically used as a tool to antagonize ERalpha signaling to study estrogen-dependent physiological processes. It has been used in studies of neuroprotection, where inhibition of ERalpha helps identify receptor subtype-specific contributions to estrogen-mediated effects in the brain. |
| Enzyme Assay |
For in vitro receptor binding assays: Incubate ERalpha protein with radiolabeled estradiol (3H-E2) at 0.5-2 nM in binding buffer (10 mM Tris-HCl, 1 mM EDTA, 10% glycerol, pH 7.4). Add varying concentrations of MPP dihydrochloride (0.1 nM to 10 uM). Incubate at 4degC overnight. Separate bound from free radioligand by charcoal dextran precipitation or filtration. Count radioactivity by scintillation. Calculate Ki and IC50 values by nonlinear regression. For ERalpha antagonist activity assays, use a luciferase reporter system with an estrogen response element (ERE).
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| Cell Assay |
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: 25 µM, 50 µM and 100 µM After 24 hrs (hours) of treatment Cell viability diminished Dramatically. However, MPP dihydrochloride at concentrations below 25 µM did not Dramatically alter cell viability. Cell proliferation assay[1] Cell Types: RL95-2 Cell Tested Concentrations: 10, 15, 20 and 25 µM Incubation Duration: 72 hrs (hours) Experimental Results: Antiproliferative activity was shown at 10 µM concentration. Western Blot Analysis[1] Cell Types: RL95-2 Cell Line Tested Concentrations: 20 µM Incubation Duration: 24 hrs (hours) Experimental Results: diminished ERα phosphorylation but did not change Akt phosphorylation. The ratio of p-ERα/ERα was diminished compared with the control group. For cell-based signaling studies: Culture ERalpha-positive cell lines (e.g., MCF-7 breast cancer cells) in phenol red-free media with charcoal-stripped serum. Treat cells with MPP dihydrochloride (0.1-10 uM) for 30-60 minutes before adding estradiol (1-10 nM). After 24 hours of treatment, assess cell viability by MTT assay or measure ERalpha target gene expression (e.g., pS2, progesterone receptor) by qRT-PCR or western blot. For primary hippocampal cell studies, treat with 1 pM to 1 uM MPP dihydrochloride for 24-48 hours before H2O2-induced oxidative stress challenge, then measure LDH activity and cell survival. |
| Animal Protocol |
Animal/Disease Models: 9-10 weeks old male C57BL/6N mice [2]
Doses: low dose (20 μg/kg body weight) or high dose (200 μg/kg body weight) Route of Administration: subcutaneous injection; injection volume 5mL/kg; Results 60 minutes before PPI test: Caused a dose-dependent decrease in PPI percentage. Pretreatment at 200 μg/kg diminished the average percentage of PPI fraction by approximately 30%. No in vivo animal protocol is standardized for MPP dihydrochloride alone. For studies involving ERalpha antagonism: Administer MPP dihydrochloride to rodents via intraperitoneal injection at doses of 0.5-5 mg/kg, typically dissolved in 10% DMSO and 90% sesame oil or saline. Inject 30 minutes to 2 hours before estradiol administration or before behavioral testing. For neuroprotection studies, administer before inducing oxidative stress or ischemic injury. Collect brain tissues for immunohistochemistry and molecular analysis. |
| ADME/Pharmacokinetics |
No detailed pharmacokinetic data is publicly available for MPP dihydrochloride. As a small molecule with molecular weight of 542.5, it is expected to have moderate oral bioavailability, but intraperitoneal administration is more commonly used in research settings. The compound is soluble in DMSO at >10 mM and should be stored as a powder at -20degC. Stock solutions can be stored below -20degC for several months.
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| Toxicity/Toxicokinetics |
No specific toxicity data is available for this ERalpha antagonist. At concentrations used in research (1 pM to 10 uM in vitro, and mg/kg doses in vivo), no overt toxicity has been reported. However, as with all research chemicals, standard laboratory safety precautions should be followed. Avoid inhalation and skin contact. Use appropriate personal protective equipment.
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| References |
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| Additional Infomation |
MPP dihydrochloride is a research-grade chemical tool intended for laboratory use only, not for diagnostic or therapeutic applications. It is widely used to study the role of ERalpha in neuroprotection, cancer, metabolism, and reproductive biology. The compound should be stored as a powder at -20degC in a dry, dark environment. It is soluble in DMSO (10-50 mM). When preparing stock solutions, warm the tube to 37degC for 10 minutes and/or shake in an ultrasonic bath as needed. No clinical trials or approved therapeutic status exist.
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| Molecular Formula |
C29H33CL2N3O3
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| Molecular Weight |
542.49662566185
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| Exact Mass |
541.189
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| CAS # |
911295-24-4
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| Related CAS # |
MPP hydrochloride;2863676-89-3;Methylpiperidino pyrazole;289726-02-9
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| PubChem CID |
135541421
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| Appearance |
White to off-white solid powder
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| LogP |
7.332
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
37
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| Complexity |
621
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
FWDNPWVVRVSJQH-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C29H31N3O3.2ClH/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;2*1H
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| Chemical Name |
4-[1-(4-hydroxyphenyl)-4-methyl-5-[4-(2-piperidin-1-ylethoxy)phenyl]pyrazol-3-yl]phenol;dihydrochloride
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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 : ~30 mg/mL (~55.30 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8433 mL | 9.2166 mL | 18.4332 mL | |
| 5 mM | 0.3687 mL | 1.8433 mL | 3.6866 mL | |
| 10 mM | 0.1843 mL | 0.9217 mL | 1.8433 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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