Canrenone-Aldadiene-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemECanrenoneCat. No.: HY-B1438CAS No.: 976-71-6Synonyms: Aldadiene; SC9376; SC14266分式: CHO分量: 340.46作靶点: Mineralocorticoid Receptor作通路: Metabolic Enzyme/Protease储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month

2、溶解性数据体外实验 DMSO : 100 mg/mL (293.72 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.9372 mL 14.6860 mL 29.3720 mL5 mM 0.5874 mL 2.9372 mL 5.8744 mL10 mM 0.2937 mL 1.4686 mL 2.9372 mL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，并请注意储备液的保存式和期限。体内实验请根据您的实验动物和给药式选择适当的溶解案，配

3、制前请先配制澄的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄的储备液可以根据储存条件，适当保存；以下溶剂前的百分指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 3 mg/mL (8.81 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 3 mg/mL (8.81 mM); Clear solution1/2 Mast

4、er of Small Molecules 您边的抑制剂师www.MedChemE3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 3 mg/mL (8.81 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Canrenone (Aldadiene; SC9376; SC14266)泛作利尿剂的醛酮 (aldosterone) 拮抗剂。IC50 & Target Target: Aldosterone 1体外研究 Canrenone inhibits the production of eortieosterone

5、, 18-hydroxydesoxyeortieosterone, 18-hydroxycorticosterone and aldosterone in a dose-dependent manner 1. Canrenone dose-dependentlyreduces platelet-derived growth factorinduced cell proliferation and motility. Canrenone inhibits the activityof the Na+/H+ exchanger 1 induced by platelet-derived growt

6、h factor 2.体内研究 Canrenone is the principal active metabolite of Spironolactone in the rat only for a limited period. Duringchronic treatment a difference developed between the effect of Spironolactone and Canrenone on the RAASindicating a decrease in the anti-mineralocorticoid activity of Canrenone

7、and an increase in the efficacy ofSpironolactone 3.PROTOCOLCell Assay 2 Confluent Hepatic Stellate Cells (HSC) are incubated in SFIF medium for 24 hours and exposed toincreasing concentrations of canrenone (1, 5, 10, 25 M). Cell viability is evaluated by the trypan blue dyeexclusion test at the end

8、of a 24- to 48-hour incubation period 2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Rats 3Administration 3 Canrenone (CAN) is given orally in two different doses (10.25, 20.5 mg/mL) to Male SPF Sprague-Dawleyrats for 6 weeks. To determine the

9、 Na+, K+, fluid and aldosterone excretion the urine of the rats destined tobe killed after 6 weeks is collected at weekly intervals 3.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Erbler HC, et al. On the mechanism of the inhibitory actio

10、n of the spirolactone SC 9376 (aldadiene) on the production of corticosteroidsin 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. 200

11、3Feb;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.McePdfHeight2/2 Master of Small Molecules 您边的抑制剂师www.MedChemECaution: Product has not b