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Megestrol acetate (BDH1298) 是具有口服活性的合成孕激素。它还具有抗雄激素特性,可用于治疗厌食症和恶病质。
Megestrol acetate (BDH1298) 是具有口服活性的合成孕激素。它还具有抗雄激素特性,可用于治疗厌食症和恶病质。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
500 mg | ¥ 339 | 现货 | |
1 g | ¥ 417 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 417 | 现货 |
产品描述 | Megestrol acetate (BDH1298) is a progestogen with actions and uses similar to those of the progestogens in general. Megestrol acetate also has anti-androgenic properties. It is given by mouth in the palliative treatment or as an adjunct to other therapy in endometrial carcinoma and in breast cancer. Megestrol acetate has been approved to treat anorexia and cachexia. |
靶点活性 | HegG2:260 μM(ec50) |
体外活性 | Megestrol acetate通过核心C/EBPβ抑制再灌注损伤引起的大鼠海马区细胞质芳香酶的表达。[1] Megestrol acetate 在剂量依赖性的方式下显著提高脂肪源性干细胞(ASCs)的增殖、迁移和成脂细胞分化。Megestrol acetate 还在ASCs中上调了糖皮质激素受体(GR)下游基因。[2] |
体内活性 | Megestrol acetate 显著降低雌二醇(E2)和睾丸素(T)在雌性鱼类或11-酮睾丸素(11-KT)在雄性鱼类的循环浓度。Megestrol acetate 接触显著抑制了下丘脑-垂体-性腺(HPG)轴沿线特定基因的转录。[3] 在猫中,经6个月及12个月的治疗后,Megestrol acetate 引起葡萄糖耐受性的逐步恶化,空腹血浆葡萄糖浓度明显升高,而血浆葡萄糖清除率则显著下降。Megestrol acetate 还逐渐降低猫静息时的血浆皮质醇浓度及ACTH刺激后的皮质醇浓度。[4] 与未经治疗的对照组相比,给药Megestrol acetate (50 mg/kg/day)9天显著增加食物和水的摄入。Megestrol acetate (50 mg/kg/day)显著(90-140%)增加大鼠弓状核(合成神经肽Y处)、外侧下丘脑区(弓状神经元投射处)以及内侧前视区、腹内侧核和背内侧核中神经肽Y的浓度。[5] |
别名 | 醋酸甲地孕酮, SC10363, BDH1298 |
分子量 | 384.51 |
分子式 | C24H32O4 |
CAS No. | 595-33-5 |
Smiles | [H][C@@]12CC[C@](OC(C)=O)(C(C)=O)[C@@]1(C)CC[C@@]1([H])[C@@]2([H])C=C(C)C2=CC(=O)CC[C@]12C |
密度 | 1.0474 g/cm3 (Estimated) |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||
溶解度信息 | Ethanol: 7.7 mg/mL (20 mM) DMSO: 10 mg/mL (26.01 mM), Sonication is recommended. | |||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||
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