| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
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| Targets |
ERα ERβ
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|---|---|
| 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].
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| 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].
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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. |
| 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%. |
| 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. [3]. Davis AM, et al. The effects of the selective estrogen receptor modulators, methyl-piperidino-pyrazole (MPP), and raloxifene in normal and cancerous endometrial cell lines and in the murine uterus. Mol Reprod Dev. 2006 Aug;73(8):1034-44. |
| Molecular Formula |
C29H32CLN3O3
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|---|---|
| Molecular Weight |
506.04
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| CAS # |
2863676-89-3
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| Related CAS # |
MPP dihydrochloride;911295-24-4
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| Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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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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