Medroxyprogesterone acetate (NSC-26386)

Catalog No.S2567 Synonyms: MPA, Medroxyprogesterone 17-acetate, Farlutin

For research use only.

Medroxyprogesterone acetate (MPA, NSC-26386, Medroxyprogesterone 17-acetate, Farlutin) is a synthetic progestin and act as a potent progesterone receptor agonist, used to treat abnormal menstruation or irregular vaginal bleeding.

Medroxyprogesterone acetate (NSC-26386) Chemical Structure

CAS No. 71-58-9

Selleck's Medroxyprogesterone acetate (NSC-26386) has been cited by 6 Publications

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Biological Activity

Description Medroxyprogesterone acetate (MPA, NSC-26386, Medroxyprogesterone 17-acetate, Farlutin) is a synthetic progestin and act as a potent progesterone receptor agonist, used to treat abnormal menstruation or irregular vaginal bleeding.
Targets
progestogen Receptor [1]
In vitro

Medroxyprogesterone acetate (MPA) inhibits the enzyme 3-hydroxyste-roid dehydrogenase, involved in the reversible conversion between 5alpha-dihydroprogesterone (DHP) and 3alpha, 5alpha-tetrahydroprogesterone (THP), and therefore may affect the local actions of DHP and THP in the brain. [1] Medroxyprogesterone acetate (MPA) reduces secretion of IL-6 and PTHrP from human breast cancer cells. MPA dose-dependently decreases the secretion and mRNA expression of IL-6 and PTHrP in the KTC-2 cells. [2] Medroxyprogesterone acetate (MPA) and dexamethasone dose dependently increases alpha-ENaC promoter-driven luciferase activity in M-1 cells, which is not inhibited by Org31710, indicating that Medroxyprogesterone acetate regulates alpha-ENaC in a PR-independent manner. Medroxyprogesterone acetate and dexamethasone, but not progesterone, dose dependently increases alpha-ENaC and sgk1 mRNA in M-1 and in Madin-Darby canine kidney-C7 cells, both collecting duct cell lines. [3] Medroxyprogesterone acetate (MPA) (0.1 nM) significantly enhances the in vitro production of specific immunoglobulin G (IgG) antibodies, an effect that appears to involve the interaction of the progestin with PRG receptors[4]

In vivo Medroxyprogesterone acetate (MPA) impairs delayed memory retention on the water radial-arm maze (WRAM), and exacerbates overnight forgetting on the Morris maze (MM) in aged ovariectomized (OVX) rats. Medroxyprogesterone acetate (MPA) significantly and progesterone marginally decreases GAD levels in the hippocampus, and both MPA and progesterone significantly increases GAD levels in the entorhinal cortex. [5]

Protocol (from reference)

Solubility (25°C)

In vitro

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
5% DMSO+30% PEG 300+5% Tween 80+ddH2O
For best results, use promptly after mixing.

0.5mg/mL

Chemical Information

Molecular Weight 386.52
Formula

C24H34O4

CAS No. 71-58-9
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1CC2C(CCC3(C2CCC3(C(=O)C)OC(=O)C)C)C4(C1=CC(=O)CC4)C

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04893798 Recruiting Combination Product: Sayana Press Healthy Pfizer September 16 2021 Phase 1
NCT03443089 Completed Drug: Test formulation|Drug: Reference formulation Contraception Galeno Desenvolvimento de Pesquisas Clínicas|Biolab Sanus Farmaceutica March 31 2017 Phase 1
NCT02509767 Completed Drug: Subcutaneous depot medroxyprogesterone acetate Contraception Planned Parenthood Federation of America|Pfizer|Tara Health Foundation August 2015 Phase 4
NCT01776203 Terminated Drug: Medroxyprogesterone 17-Acetate Dysfunctional Uterine Bleeding Kaiser Permanente January 2012 Phase 4

(data from https://clinicaltrials.gov, updated on 2022-08-01)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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