GLPBio

Medroxyprogesterone acetate

Catalog No.: GC12974Purity:>99.50%Synonyms: NSC 21171, NSC 26386, U-8839
Medroxyprogesterone acetate (MPA) is a synthetic progestin.

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Medroxyprogesterone acetate
Cas No.: 71-58-9
10mM (in 1mL DMSO)In Stock
$35.00
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100mgIn Stock
$32.00
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500mgIn Stock
$56.00
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Description

Medroxyprogesterone acetate (MPA) is a synthetic progestin[1]. Medroxyprogesterone acetate can be used for contraception, endometriosis, endometrial bleeding, and can also be used to treat endometrial cancer and breast cancer[2, 3].

In vitro, treatment of human colon cancer cell lines HT29 and HCT116 cells with Medroxyprogesterone acetate (20nM) for 48h reduced the level of cyclin E and led to G1 phase arrest of cells[4]. Treatment of human endothelial cells with Medroxyprogesterone acetate (0.5, 10nM) for 16h inhibited the expression of intercellular adhesion molecule 1 (ICAM-1) and vascular cell adhesion molecule 1 (VCAM-1), and reduced the adhesion of endothelial cells to leukocytes[5].

In vivo, oral treatment of ovariectomized mice with Medroxyprogesterone acetate (0.05, 0.1, and 0.2mg/kg/day) for 14 days increased allopregnanolone levels in all tissues except the adrenal glands and affected β-END levels in the hippocampus and interneuronal lobe[6]. Intramuscular treatment of mice with KPL-4 cell xenografts with Medroxyprogesterone acetate (100mg/kg) significantly reduced serum IL-6 levels but did not affect tumor growth[7].

References:
[1] Mattson R H, Cramer J A, Caldwell B V, et al. Treatment of seizures with medroxyprogesterone acetate: preliminary report[J]. Neurology, 1984, 34(9): 1255-1255.
[2] Kaunitz A M. Long-acting injectable contraception with depot medroxyprogesterone acetate[J]. American journal of obstetrics and gynecology, 1994, 170(5): 1543-1549.
[3] Kim J J, Kurita T, Bulun S E. Progesterone action in endometrial cancer, endometriosis, uterine fibroids, and breast cancer[J]. Endocrine reviews, 2013, 34(1): 130-162.
[4] Tanaka Y, Kato K, Mibu R, et al. Medroxyprogesterone acetate inhibits proliferation of colon cancer cell lines by modulating cell cycle-related protein expression[J]. Menopause, 2008, 15(3): 442-453.
[5] Simoncini T, Mannella P, Fornari L, et al. Differential signal transduction of progesterone and medroxyprogesterone acetate in human endothelial cells[J]. Endocrinology, 2004, 145(12): 5745-5756.
[6] Bernardi F, Pluchino N, Pieri M, et al. Progesterone and medroxyprogesterone acetate effects on central and peripheral allopregnanolone and beta-endorphin levels[J]. Neuroendocrinology, 2006, 83(5-6): 348-359.
[7] Kurebayashi J, Yamamoto S, Otsuki T, et al. Medroxyprogesterone acetate inhibits interleukin 6 secretion from KPL-4 human breast cancer cells both in vitro and in vivo: a possible mechanism of the anticachectic effect[J]. British journal of cancer, 1999, 79(3): 631-636.

Protocol

Cell experiment [1]:

Cell lines

HT29、HCT116 cells

Preparation Method

Cells were plated on 10-cm dishes at a density of 1×106/well. After 24h, the cells were stimulated in phenol red-free medium containing 10% charcoal treated fetal bovine serum supplemented with 20nM Medroxyprogesterone acetate (MPA) or vehicle. After 48h, the cells were washed twice with cold phosphate-buffered saline and then lysed with RIPA buffer and protease inhibitor cocktail. The samples were electrophoresed and transferred onto a nitrocellulose membrane. The membranes were immunoblotted with anti-cyclin D1 antibody and anti-cyclin E antibody and analyzed by using an ECL Western blotting detection kit.

Reaction Conditions

20nM; 48h

Applications

Medroxyprogesterone acetate decreases the level of cyclin E, contributing to the G1 arrest in HT29 and HCT116 cells.

Animal experiment [2]:

Animal models

Female Wistar rats

Preparation Method

Thirteen groups of Wistar ovariectomized rats received one of the following treatments: oral Progesterone (2, 4 or 8mg/kg/day); oral Medroxyprogesterone acetate (0.05, 0.1 or 0.2mg/kg/day); Estradiol valerate (0.05mg/kg/day); Estradiol valerate+progesterone (0.05mg/kg/day+2, 4 or 8mg/kg/day), or Estradiol valerate+Medroxyprogesterone acetate (0.05mg/kg/day+0.05, 0.1 or 0.2mg/kg/day) for 14 days. One group of fertile and one group of ovariectomized rats were used as controls. The concentration of allopregnanolone was assessed in the frontal and parietal lobes, hypothalamus, hippocampus, anterior pituitary, adrenals and serum, while the beta-END content was assessed in the frontal and parietal lobes, hypothalamus, hippocampus, anterior and neurointermediate pituitary, and plasma.

Dosage form

0.05, 0.1, 0.2mg/kg/day for 14 days; p.o.

Applications

Medroxyprogesterone acetate increased allopregnanolone levels in all tissues except the adrenal glands. Medroxyprogesterone acetate only affected β-END levels in the hippocampus and interneuronal lobe.

References:
[1]Tanaka Y, Kato K, Mibu R, et al. Medroxyprogesterone acetate inhibits proliferation of colon cancer cell lines by modulating cell cycle-related protein expression[J]. Menopause, 2008, 15(3): 442-453.
[2]Bernardi F, Pluchino N, Pieri M, et al. Progesterone and medroxyprogesterone acetate effects on central and peripheral allopregnanolone and beta-endorphin levels[J]. Neuroendocrinology, 2006, 83(5-6): 348-359.

Product Documents

Purity:>99.50%Appearance:A solid

Chemical Properties

CAS No.
71-58-9
Synonyms
NSC 21171, NSC 26386, U-8839
Chemical Name
[(6S,8R,9S,10R,13S,14S,17R)-17-acetyl-6,10,13-trimethyl-3-oxo-2,6,7,8,9,11,12,14,15,16-decahydro-1H-cyclopenta[a]phenanthren-17-yl] acetate
SMILES
CC1CC2C(CCC3(C2CCC3(C(=O)C)OC(=O)C)C)C4(C1=CC(=O)CC4)C
Molecular Formula
C24H34O4
Molecular Weight
386.52
Solubility
≥ 9.5mg/mL in DMSO with gentle warming
Storage
Store at 4°C
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.

CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility

g/mol

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