Medroxyprogesterone acetate
(Synonyms: 醋酸甲羟孕酮; Medroxyprogesterone 17-acetate; Farlutin) 目录号 : GC12974
Medroxyprogesterone acetate（MPA）是一种人工合成的孕激素。
Cas No.:71-58-9
Sample solution is provided at 25 µL, 10mM.
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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.
Medroxyprogesterone acetate（MPA）是一种人工合成的孕激素[1]。Medroxyprogesterone acetate能够用于避孕、子宫内膜异位症、子宫内膜出血，还能够用于治疗子宫内膜癌、乳腺癌[2, 3]。
在体外，Medroxyprogesterone acetate（20nM）处理人结肠癌细胞系HT29和HCT116细胞48h，降低了细胞周期蛋白E的水平，导致了细胞的G1期停滞[4]。Medroxyprogesterone acetate（0.5、10nM）处理人内皮细胞16h，抑制了细胞间粘附分子 1（ICAM-1）和血管细胞粘附分子 1（VCAM-1）表达，降低了内皮细胞对白细胞的粘附性[5]。
在体内，Medroxyprogesterone acetate（0.05, 0.1, 0.2mg/kg/day）通过口服治疗做了卵巢切除手术的小鼠14天，增加了除肾上腺外的所有组织中的异孕酮水平，影响了海马和神经中间叶的β-END水平[6]。Medroxyprogesterone acetate（100mg/kg）通过肌肉注射治疗KPL-4细胞异种移植小鼠，显著降低了血清 IL-6水平，但不影响肿瘤生长[7]。
| 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: | |
| Cas No. | 71-58-9 | SDF | |
| 别名 | 醋酸甲羟孕酮; Medroxyprogesterone 17-acetate; Farlutin | ||
| 化学名 | [(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 | ||
| Canonical SMILES | CC1CC2C(CCC3(C2CCC3(C(=O)C)OC(=O)C)C)C4(C1=CC(=O)CC4)C | ||
| 分子式 | C24H34O4 | 分子量 | 386.52 |
| 溶解度 | ≥ 9.5mg/mL in DMSO with gentle warming | 储存条件 | Store at 4°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.5872 mL | 12.9359 mL | 25.8719 mL |
| 5 mM | 0.5174 mL | 2.5872 mL | 5.1744 mL |
| 10 mM | 0.2587 mL | 1.2936 mL | 2.5872 mL |
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动物平均体重 | g | |
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动物数量 | 只 |
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- Purity: >99.50%
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