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Canrenone (Synonyms: Aldadiene, NSC 261713, SC-9376, SC-14266)

Catalog No.GC17537

Mineralocorticoid receptor antagonist

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Canrenone Chemical Structure

Cas No.: 976-71-6

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50mg
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Protocol

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.
[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.

Background

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.

Chemical Properties

Cas No. 976-71-6 SDF
Synonyms Aldadiene, NSC 261713, SC-9376, SC-14266
Chemical Name (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
Formula C22H28O3 M.Wt 340.46
Solubility DMF: 30 mg/ml,DMSO: 30 mg/ml,DMSO:PBS(pH 7.2) (1:4): 0.2 mg/ml,Ethanol: 10 mg/ml Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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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
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Average Rating: 5 ★★★★★ (Based on Reviews and 37 reference(s) in Google Scholar.)

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