Canrenone-Aldadiene-DataSheet-生命科學(xué)試劑-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作靶點(diǎn): Mineralocorticoid Receptor作通路: Metabolic Enzyme/Protease儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month

2、溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 100 mg/mL (293.72 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液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請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。體內(nèi)實(shí)驗(yàn)請根據(jù)您的實(shí)驗(yàn)動物和給藥式選擇適當(dāng)?shù)娜芙獍?，?/p>

3、制前請先配制澄的儲備液，再依次添加助溶劑(為保證實(shí)驗(yàn)結(jié)果的可靠性，體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使；澄的儲備液可以根據(jù)儲存條件，適當(dāng)保存；以下溶劑前的百分指該溶劑在您配制終溶液中的體積占)：1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 3 mg/mL (8.81 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 3 mg/mL (8.81 mM); Clear solution1/2 Mast

4、er of Small Molecules 您邊的抑制劑師www.MedChemE3. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 3 mg/mL (8.81 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Canrenone (Aldadiene; SC9376; SC14266)泛作利尿劑的醛酮 (aldosterone) 拮抗劑。IC50 & Target Target: Aldosterone 1體外研究 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.體內(nèi)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 您邊的抑制劑師www.MedChemECaution: Product has not b