Canrenone
(Synonyms: 坎利酮,Aldadiene; SC9376) 目录号 : GC17537An Analytical Reference Standard
Cas No.:976-71-6
Sample solution is provided at 25 µL, 10mM.
Canrenone (Aldadiene; SC9376; SC14266) is an aldosterone antagonist extensively used as a diuretic agent.
Canrenone inhibits the production of eortieosterone, 18-hydroxydesoxyeortieosterone, 18-hydroxycorticosterone and aldosterone in a dose-dependent manner[1]. Canrenone dose-dependently reduces platelet-derived growth factor–induced cell proliferation and motility. Canrenone inhibits the activity of the Na+/H+ exchanger 1 induced by platelet-derived growth factor[2].
Canrenone is the principal active metabolite of Spironolactone in the rat only for a limited period. During chronic treatment a difference developed between the effect of Spironolactone and Canrenone on the RAAS indicating a decrease in the anti-mineralocorticoid activity of Canrenone and an increase in the efficacy of Spironolactone[3].
References:
[1]. Erbler HC, et al. On the mechanism of the inhibitory action of the spirolactone SC 9376 (aldadiene) on the production of corticosteroids in rat adrenals in vitro. Naunyn Schmiedebergs Arch Pharmacol. 1973;277(2):139-49.
[2]. Caligiuri A, et al. Antifibrogenic effects of canrenone, an antialdosteronic drug, on human hepatic stellate cells. Gastroenterology. 2003 Feb;124(2):504-20.
[3]. Erbler HC, et al. Effect of spironolactone and its main metabolite canrenone on the renin-angiotensin-aldosterone-system during long-term treatment in rats. Acta Endocrinol (Copenh). 1979 Jan;90(1):147-56.
Cell experiment: |
Confluent Hepatic Stellate Cells (HSC) are incubated in SFIF medium for 24 hours and exposed to increasing concentrations of canrenone (1, 5, 10, 25 μM). Cell viability is evaluated by the trypan blue dye exclusion test at the end of a 24- to 48-hour incubation period[2]. |
Animal experiment: |
Rats[3]Canrenone (CAN) is given orally in two different doses (10.25, 20.5 mg/mL) to Male SPF Sprague-Dawley rats for 6 weeks. To determine the Na+, K+, fluid and aldosterone excretion the urine of the rats destined to be killed after 6 weeks is collected at weekly intervals[3]. |
References: [1]. Erbler HC, et al. On the mechanism of the inhibitory action of the spirolactone SC 9376 (aldadiene) on the production of corticosteroids in rat adrenals in vitro. Naunyn Schmiedebergs Arch Pharmacol. 1973;277(2):139-49. |
Cas No. | 976-71-6 | SDF | |
别名 | 坎利酮,Aldadiene; SC9376 | ||
化学名 | (2'R,8R,9S,10R,13S,14S)-10,13-dimethyl-1,8,9,10,11,12,13,14,15,16-decahydro-3'H-spiro[cyclopenta[a]phenanthrene-17,2'-furan]-3,5'(2H,4'H)-dione | ||
Canonical SMILES | O=C1O[C@]2(CC1)[C@]3(C)[C@@H](CC2)[C@H](C=C4)[C@@H]([C@](CC5)(C)C4=CC5=O)CC3 | ||
分子式 | C22H28O3 | 分子量 | 340.46 |
溶解度 | DMF: 30 mg/ml,DMSO: 30 mg/ml,DMSO:PBS(pH 7.2) (1:4): 0.2 mg/ml,Ethanol: 10 mg/ml | 储存条件 | Store at -20°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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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 2.9372 mL | 14.686 mL | 29.372 mL |
5 mM | 0.5874 mL | 2.9372 mL | 5.8744 mL |
10 mM | 0.2937 mL | 1.4686 mL | 2.9372 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
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% DMSO % % Tween 80 % saline | ||||||||||
计算重置 |
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,
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 saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet