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Spironolactone

MCE China：Spironolactone

Brand：MedChemExpress (MCE)

Cat. No.HY-B0561

CAS：52-01-7

Synonyms：SC9420

Purity：99.66%

Storage：Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months

Shipping：Room temperature in continental US; may vary elsewhere.

Description：Spironolactone is an aldosterone antagonist that acts on the aldosterone mineralocorticoid receptor (IC50=24 nM) and androgen receptor (IC50=77 nM), promotes podocyte autophagy and regulates pain. Spironolactone improves hypertension-related vascular hypertrophy and remodeling by reducing angiotensin II (AngⅡ)-induced inflammation, reduces aldosterone-induced vascular and soft tissue calcification through PIT1-dependent signaling, and alleviates vascular dysfunction in type Ⅱ diabetic mice by reducing oxidative stress and restoring NO/GC signaling; at low concentrations, it and its metabolites can interfere with aldosterone biosynthesis in the adrenal cortex and inhibit voltage-dependent Ca2+ channels to exert antihypertensive effects.

In Vitro：Spironolactone significantly inhibits Ang Ⅱ-mediated ERK and AKT phosphorylation in A7r5 cells without affecting EGFR phosphorylation[1]. Spironolactone increases PIT1 expression in human aortic smooth muscle cells in a dose-dependent manner and reverses the effects of aldosterone[2]. Spironolactone (0, 100 nM, 1 µM, 10 µM, 30 min) inhibits AngⅡ-induced inflammation[5]. Spironolactone increases the expression of podocyte-specific markers WT1 and NPHS2 and autophagy markers Beclin1 and LC3B, promoting cell autophagy[10].

In Vivo：Spironolactone blocks aldosterone (ALDO) and restores vascular remodeling caused by long-term enhancement of the renin-angiotensin system (RAS)[1]. Spironolactone (80 mg/L, p.o.) extends the lifespan of mesothelin mutant mice and reduces aldosterone-induced vascular and soft tissue calcification[2]. Spironolactone (10-80 mg/mL, subcutaneous injection) increases pain behavior in a dose-dependent manner in Male Swiss albino mice thermal and electrical pain models, but reduces inflammatory visceral pain caused by intraperitoneal acetic acid and chemical pain caused by plantar capsaicin[3]. Spironolactone (50 mg/kg, once a day for 6 weeks, oral administration) can reduce diabetes-related vascular oxidative stress and prevent vascular dysfunction by increasing the expression of antioxidant enzymes and soluble guanidyl cyclase (sGC)[4]. Spironolactone (40 mg/kg, daily, 8 weeks，i.g.) reduces urinary albumin excretion, blood lipids and fasting blood glucose levels, alleviates renal damage, promotes autophagy and reduces podocyte loss[10].

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References：

[1]. Sachiko Sakurabayashi-Kitade , et al. Aldosterone blockade by Spironolactone improves the hypertensive vascular hypertrophy and remodeling in angiotensin II overproducing transgenic mice. Atherosclerosis. 2009 Sep;206(1):54-60.  [Content Brief]

[2]. Jakob Voelkl , et al. Spironolactone ameliorates PIT1-dependent vascular osteoinduction in klotho-hypomorphic mice. J Clin Invest. 2013 Feb;123(2):812-22.  [Content Brief]

[3]. Omar M E Abdel-Salam, et al. Effect of spironolactone on pain responses in mice. EXCLI J. 2010 Feb 25:9:46-57.  [Content Brief]

[4]. Marcondes A B Silva, et al. Spironolactone treatment attenuates vascular dysfunction in type 2 diabetic mice by decreasing oxidative stress and restoring NO/GC signaling. Front Physiol. 2015 Oct 5:6:269.  [Content Brief]

[5]. Ryuzea Miura, et al. Anti-inflammatory effect of spironolactone on human peripheral blood mononuclear cells. J Pharmacol Sci. 2006 Jul;101(3):256-9.  [Content Brief]

[6]. S C Cheng, et al. Effects of Spironolactone, Canrenone and Canrenoate-K on Cytochrome P450, and 11β- and 18-Hydroxylation in Bovine and Human Adrenal Cortical Mitochondria1. Endocrinology. 1976 Oct;99(4):1097-106.  [Content Brief]

[7]. R Sorrentino. Effect of Spironolactone and Its Metabolites on Contractile Property of Isolated Rat Aorta Rings. J Cardiovasc Pharmacol. 2000 Aug;36(2):230-5.  [Content Brief]

[8]. Kim GK, et al. Oral Spironolactone in Post-teenage Female Patients with Acne Vulgaris: Practical Considerations for the Clinician Based on Current Data and Clinical Experience. J Clin Aesthet Dermatol. 2012;5(3):37-50.  [Content Brief]

[9]. Fagart J, et al. A new mode of mineralocorticoid receptor antagonism by a potent and selective nonsteroidal molecule. J Biol Chem. 2010;285(39):29932-29940.  [Content Brief]

[10]. Dong D, et al. Spironolactone alleviates diabetic nephropathy through promoting autophagy in podocytes. Int Urol Nephrol. 2019;51(4):755-764.  [Content Brief]