Medroxyprogesterone acetate
产品说明书
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同义名 : | 醋酸甲羟孕酮 ;Medroxyprogesterone 17-acetate;Farlutin;U-8839;NSC 21171;NSC-26386;MPA |
| CAS号 : | 71-58-9 | |
| 货号 : | A306697 | |
| 分子式 : | C24H34O4 | |
| 纯度 : | 99+% | |
| 分子量 : | 386.524 | |
| MDL号 : | MFCD00010483 | |
| 存储条件： |
粉末 Sealed in dry,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 9 mg/mL(23.28 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO 无水乙醇: 6 mg/mL(15.52 mM)，配合低频超声，并水浴加热至45℃助溶，注意：无水乙醇开封后，易挥发，也会吸收空气中的水分，导致溶解能力下降，请避免使用开封较久的乙醇 |
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| 动物实验配方： |
IP 2% DMSO+2% Tween80+30% PEG300+water 0.5 mg/mL clear PO 0.5% CMC-Na 35 mg/mL suspension |
| 生物活性 | |||
|---|---|---|---|
| 描述 | Progesterone Receptor (PGR) is a member or the steroid receptor superfamily. It mediates the physiological effects of progesterone, which plays a central role in reproductive events associated with the establishment and maintenance of pregnancy. Progesterone Receptor is involved in the regulation of eukaryotic gene expression and affect cellular proliferation and differentiation in target tissues. Depending on the isoform, progesterone receptor functions as transcriptional activator or repressor. The glucocorticoid receptor (GR) has a dual mode of action: as a transcription factor that binds to glucocorticoid response elements (GRE), both for nuclear and mitochondrial DNA, and as a modulator of other transcription factors. The glucocorticoid receptor affects inflammatory responses, cellular proliferation and differentiation in target tissues. The glucocorticoid receptor is involved in chromatin remodeling, plays a role in rapid mRNA degradation. The glucocorticoid receptor could also act as a coactivator for STAT5-dependent transcription upon growth hormone stimulation. Medroxyprogesterone acetate is a progestin, a synthetic variant of the human hormone progesterone. Medroxyprogesterone acetate acts as a ligand that binds to progesterone receptor. Reports also suggested that Medroxyprogesterone acetate also binds the glucocorticoid receptor. The details were that Medroxyprogesterone acetate dose dependently increased α-ENaC promoter-driven luciferase activity in M-1 cells, indicating that Medroxyprogesterone acetate regulates α-ENaC in a progesterone receptor-independent manner. Moreover, when tested in HT29 cells, Medroxyprogesterone acetate could only stimulate α-ENaC-driven reporter activity when glucocorticoid receptor was coexpressed[3]. According to another report, thyroid cancer KTC-2 cells incubated with 10-1000 nM Medroxyprogesterone acetate for 2 days showed decreased secretion and mRNA expression of IL-6 and PTHrP in a dose-dependent manner. The finding that KTC-2 cells express glucocorticoid receptor but not progesterone receptor suggested that the effect of Medroxyprogesterone acetate was mediated by glucocorticoid receptor[4]. In a rabbit model of flank wounds, Medroxyprogesterone administrated i.m. at the dose of 35 mg/kg daily prolonged the latent phase of wound healing, slowed the rate and decreased the total amount of contracture[5]. According to a published study evaluating the mnemonic and neurobiological effects of Medroxyprogesterone acetate in surgically menopausal rats, Medroxyprogesterone acetate was given at the low dose of 14 mg or the high dose of 21 mg via implanted Alzet osmotic pumps, which slowly released the agent in vivo. The results were that both doses of Medroxyprogesterone acetate impaired learning. High dose of Medroxyprogesterone acetate impaired delayed memory retention and exacerbated overnight forgetting. Medroxyprogesterone acetate treatment also significantly decreased GAD levels in the hippocampus and significantly increased GAD levels in the entorhinal cort[6]. | ||
| 临床研究 | |||||
|---|---|---|---|---|---|
| NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
| NCT03196492 | - | Recruiting | June 14, 2019 | United States, Maryland ... 展开 >> Johns Hopkins Hospital Recruiting Baltimore, Maryland, United States, 21205 Contact: Okonkwo 收起 << | |
| NCT00000897 | HIV Infections | Not Applicable | Completed | - | United States, California ... 展开 >> San Francisco AIDS Clinic / San Francisco Gen Hosp San Francisco, California, United States, 941102859 United States, Florida Univ of Florida Health Science Ctr / Pediatrics Jacksonville, Florida, United States, 32209 United States, New York Children's Hosp at Albany Med Ctr Albany, New York, United States, 12208 SUNY / Erie County Med Ctr at Buffalo Buffalo, New York, United States, 14215 United States, North Carolina Univ of North Carolina Chapel Hill, North Carolina, United States, 275997215 United States, Washington Univ of Washington Seattle, Washington, United States, 98104 收起 << |
| NCT00370019 | Premature Ovarian Failure | Phase 2 | Withdrawn | - | United States, Maryland ... 展开 >> National Institutes of Health Clinical Center, 9000 Rockville Pike Bethesda, Maryland, United States, 20892 收起 << |
| 实验方案 | |||
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| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.59mL 0.52mL 0.26mL |
12.94mL 2.59mL 1.29mL |
25.87mL 5.17mL 2.59mL |
| 参考文献 |
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