Medroxyprogesterone Acetate (MPA)

CatalogusnummerS2567 Batch:S256706

Afdrukken

Technische gegevens

Formule

C24H34O4
Moleculair gewicht 386.52 CAS-nr. 71-58-9
Oplosbaarheid (25°C)* In vitro DMSO 18 mg/mL (46.56 mM)
Ethanol 15 mg/mL (38.8 mM)
Water Insoluble
In vivo (Voeg oplosmiddelen afzonderlijk en in volgorde toe aan het product.)
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution
5%DMSO 30%PEG300 5%Tween80 60%ddH2O

Gevalideerd door Selleck labs. Mocht u aanpassingen aan deze formulering nodig hebben, neem dan contact op met ons verkoopteam voor maatwerktesten.

 0.500mg/ml (1.29mM) Taking the 1 mL working solution as an example, add 50 μL of 10 mg/ml clarified DMSO stock solution to 300 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 600 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml betekent licht oplosbaar of onoplosbaar.
* Houd er rekening mee dat Selleck de oplosbaarheid van alle verbindingen intern test en de werkelijke oplosbaarheid enigszins kan afwijken van gepubliceerde waarden. Dit is normaal en is te wijten aan lichte batch-tot-batch variaties.
* Verzending op kamertemperatuur (Stabiliteitstests tonen aan dat dit product zonder koelmaatregelen kan worden verzonden.)

Voorbereiden van stamoplossingen

Biologische activiteit

Beschrijving MPA (Medroxyprogesteronacetaat) is een synthetisch progestageen en werkt als een potente Progesterone Receptor-agonist, gebruikt voor de behandeling van abnormale menstruatie of onregelmatig vaginaal bloedverlies.
Doelen
progestogen Receptor
In vitro

Medroxyprogesterone acetate (MPA) inhibits the enzyme 3-hydroxysteroid 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.

It reduces secretion of IL-6 and PTHrP from human breast cancer cells. This compound dose-dependently decreases the secretion and mRNA expression of IL-6 and PTHrP in the KTC-2 cells.

MPA and dexamethasone dose dependently increase alpha-ENaC promoter-driven luciferase activity in M-1 cells, which is not inhibited by Org31710, indicating that it regulates alpha-ENaC in a PR-independent manner. This compound and dexamethasone, but not progesterone, dose dependently increase alpha-ENaC and sgk1 mRNA in M-1 and in Madin-Darby canine kidney-C7 cells, both collecting duct cell lines.

At 0.1 nM, it 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
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. It significantly and progesterone marginally decreases GAD levels in the hippocampus, while both MPA and progesterone significantly increase GAD levels in the entorhinal cortex.

Protocol (uit referentie)

Celassay:

[6]
  • Cellijnen

    ISK cells

  • Concentraties

    29.3 µM

  • Incubatietijd

    48 h

  • Methode

    Cells were treated with various concentrations of MPA (Medroxyprogesterone acetate) for 48 h.
Dierstudie:

[1]
  • Dierlijke modellen

    Wistar albino female rats

  • Doseringen

    1, 2, 4, or 8 mg/kg

  • Toediening

    i.p.

Referenties

  • https://pubmed.ncbi.nlm.nih.gov/16758493/
  • https://pubmed.ncbi.nlm.nih.gov/12729473/
  • https://pubmed.ncbi.nlm.nih.gov/16189295/
  • https://pubmed.ncbi.nlm.nih.gov/11576224/
  • https://pubmed.ncbi.nlm.nih.gov/20074654/
  • https://pubmed.ncbi.nlm.nih.gov/33937078/

Klantproductvalidatie

The analgesic effect of koumine was reversed in sciatic nerve chronic constriction injury rats by intrathecal treatment with medroxyprogesterone acetate. Medroxyprogesterone acetate (MPA) or dimethyl sulfoxide (DMSO, vehicle) was administered via an intrathecal catheter 10 days after sciatic nerve chronic constriction injury (CCI) surgery. After 30 min, koumine (7 mg kg−1 bw) or normal saline (NS) was administered by subcutaneous (s.c.) injection. The mechanical withdrawal threshold (MWT) of the hind paws was measured 1 h after completion of the drug or vehicle administration. The data are presented as the mean ± SEM (n = 6 per group) and were analyzed by one-way ANOVA followed by Bonferroni post hoc test at each time point. *P < 0.05 vs. the DMSO + NS group; # P < 0.05 vs. the DMSO + koumine group.

Gegevens van [ , , Molecular Pain, 2015, 11:46. ]

Selleck's Medroxyprogesterone Acetate (MPA) Is geciteerd door 16 Publicaties

Steroid-Modulated Transcription Synergistically Forms DNA Double-Strand Breaks With Topoisomerase II Inhibitor [ Cancer Sci, 2025, 10.1111/cas.70081] PubMed: 40231641
Investigating Aging-Related Endometrial Dysfunction Using Endometrial Organoids [ Cell Prolif, 2024, e13780.] PubMed: 39695355
Deficiency of UCHL1 results in insufficient decidualization accompanied by impaired dNK modulation and eventually miscarriage [ J Transl Med, 2024, 22(1):478] PubMed: 38769534
Inhibition of the transmembrane transporter ABCB1 overcomes resistance to doxorubicin in patient-derived organoid models of HCC [ Hepatol Commun, 2024, 8(5)e0437] PubMed: 38696353
The role of non-genomic actions of progesterone and its membrane receptor agonist in ovarian cancer cell death [ Cancer Rep (Hoboken), 2024, 7(1):e1934] PubMed: 38013666
Genome-wide CRISPR screening reveals ADCK3 as a key regulator in sensitizing endometrial carcinoma cells to MPA therapy [ Br J Cancer, 2023, 129(4):601-611] PubMed: 37402867
Elevated high-mannose N-glycans hamper endometrial decidualization [ iScience, 2023, 10.1016/j.isci.2023.108170] PubMed: 37915610
RNA-seq and ATAC-seq analysis of CD163+ macrophage-induced progestin-insensitive endometrial cancer cells [ Cancer Med, 2023, 12(5):5964-5978] PubMed: 36373483
Long-Acting Technologies for Prevention of HIV and Unplanned Pregnancy [ ProQuest, 2023, 30314559] PubMed: none
ABX-1431 inhibits the development of endometrial adenocarcinoma and reverses progesterone resistance by targeting MGLL [ Cell Death Dis, 2022, 13(12):1067] PubMed: 36550099

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NIET VOOR HUMANE, VETERINAIRE DIAGNOSTISCHE OF THERAPEUTISCHE DOELEINDEN.