规格 | 价格 | 库存 | 数量 |
---|---|---|---|
500mg |
|
||
1g |
|
||
2g |
|
||
5g |
|
||
10g |
|
||
50g |
|
||
Other Sizes |
|
体外研究 (In Vitro) |
在 MCF7/ADR 细胞系中,单独使用醋酸甲地孕酮会导致 ICKY 为 48.7 p,M[2]。
|
---|---|
体内研究 (In Vivo) |
当以 100 或 300 mg/kg 的剂量每天皮下注射连续 7 天时,醋酸甲地孕酮可以减轻 MAC16 肿瘤和 TNF 带来的体重减轻[1]。
|
动物实验 |
Animal/Disease Models: Pure strain female NMRI mice (age 6 to 8 weeks)[1].
Doses: 100 or 300 mg/kg (50 mg megestrol acetate was suspended in 3 ml of pure corn oil). Route of Administration: subcutaneously (sc) daily over a 7-day period. Experimental Results: Produced a highly significant reversal of the TNF-induced decrease in body weight, accompanied by a significant increase in both food and water intake. Caused an increase in body weight over a 24-hour period to female NMRI mice. No effect on blood glucose levels in saline controls, concurrent Administration of megestrol acetate with TNF caused a significant increase in blood glucose compared with administration of TNF alone. Caused a dose-related reduction in the loss of host body weight in animals bearing the MAC16 tumour. |
参考文献 |
[1]. S A Beck, et al. Effect of megestrol acetate on weight loss induced by tumour necrosis factor alpha and a cachexia-inducing tumour (MAC16) in NMRI mice. Br J Cancer. 1990 Sep;62(3):420-4.
[2]. L Panasci, et al. Sensitization to doxorubicin resistance in breast cancer cell lines by tamoxifen and megestrol acetate. Biochem Pharmacol. 1996 Oct 11;52(7):1097-102. [3]. J Geller, et al. Acute therapy with megestrol acetate decreases nuclear and cytosol androgen receptors in human BPH tissue. Prostate. 1982;3(1):11-5. [4]. J H von Roenn, et al. Megestrol acetate for treatment of cachexia associated with human immunodeficiency virus (HIV) infection. Ann Intern Med. 1988 Nov 15;109(10):840-1. [5]. Vincenzo Musolino, et al. Megestrol acetate improves cardiac function in a model of cancer cachexia-induced cardiomyopathy by autophagic modulation. J Cachexia Sarcopenia Muscle. 2016 Dec;7(5):555-566. |
分子式 |
C24H32O4
|
|
---|---|---|
分子量 |
384.51
|
|
CAS号 |
595-33-5
|
|
相关CAS号 |
Megestrol acetate-d3;162462-72-8;Megestrol;3562-63-8;Megestrol acetate-d3-1
|
|
SMILES |
O(C(C([H])([H])[H])=O)[C@]1(C(C([H])([H])[H])=O)C([H])([H])C([H])([H])[C@@]2([H])[C@]3([H])C([H])=C(C([H])([H])[H])C4=C([H])C(C([H])([H])C([H])([H])[C@]4(C([H])([H])[H])[C@@]3([H])C([H])([H])C([H])([H])[C@@]21C([H])([H])[H])=O
|
|
InChi Key |
RQZAXGRLVPAYTJ-GQFGMJRRSA-N
|
|
InChi Code |
InChI=1S/C24H32O4/c1-14-12-18-19(22(4)9-6-17(27)13-21(14)22)7-10-23(5)20(18)8-11-24(23,15(2)25)28-16(3)26/h12-13,18-20H,6-11H2,1-5H3/t18-,19+,20+,22-,23+,24+/m1/s1
|
|
化学名 |
(8R,9S,10R,13S,14S,17R)-17-acetyl-6,10,13-trimethyl-3-oxo-2,3,8,9,10,11,12,13,14,15,16,17-dodecahydro-1H-cyclopenta[a]phenanthren-17-yl acetate
|
|
别名 |
|
|
存储方式 |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
|
运输条件 |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
溶解度 (体外) |
|
|||
---|---|---|---|---|
溶解度 (体内) |
Solubility in Formulation 1: ≥ 2 mg/mL (5.20 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2 mg/mL (5.20 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2 mg/mL (5.20 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. 1、请先配制澄清的储备液(如:用DMSO配置50 或 100 mg/mL母液(储备液)); 2、取适量母液,按从左到右的顺序依次添加助溶剂,澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明,并不一定代表此产品 的实际溶解配方): 10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline); 假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀/澄清;向上述体系中加入50 μL Tween-80,混合均匀/澄清;然后继续加入450 μL ddH2O (或 saline)定容至 1 mL; 3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例; 4、 如产品在配制过程中出现沉淀/析出,可通过加热(≤50℃)或超声的方式助溶; 5、为保证最佳实验结果,工作液请现配现用! 6、如不确定怎么将母液配置成体内动物实验的工作液,请查看说明书或联系我们; 7、 以上所有助溶剂都可在 Invivochem.cn网站购买。 |
制备储备液 | 1 mg | 5 mg | 10 mg | |
1 mM | 2.6007 mL | 13.0036 mL | 26.0071 mL | |
5 mM | 0.5201 mL | 2.6007 mL | 5.2014 mL | |
10 mM | 0.2601 mL | 1.3004 mL | 2.6007 mL |
1、根据实验需要选择合适的溶剂配制储备液 (母液):对于大多数产品,InvivoChem推荐用DMSO配置母液 (比如:5、10、20mM或者10、20、50 mg/mL浓度),个别水溶性高的产品可直接溶于水。产品在DMSO 、水或其他溶剂中的具体溶解度详见上”溶解度 (体外)”部分;
2、如果您找不到您想要的溶解度信息,或者很难将产品溶解在溶液中,请联系我们;
3、建议使用下列计算器进行相关计算(摩尔浓度计算器、稀释计算器、分子量计算器、重组计算器等);
4、母液配好之后,将其分装到常规用量,并储存在-20°C或-80°C,尽量减少反复冻融循环。
计算结果:
工作液浓度: mg/mL;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL)。如该浓度超过该批次药物DMSO溶解度,请首先与我们联系。
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL ddH2O,混匀澄清。
(1) 请确保溶液澄清之后,再加入下一种溶剂 (助溶剂) 。可利用涡旋、超声或水浴加热等方法助溶;
(2) 一定要按顺序加入溶剂 (助溶剂) 。