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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.
For research use only. We do not sell to patients.
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[1][2][3][4][5][6][7][8][9][10].
Cellular Effect
Cell Line
Type
Value
Description
References
CHO-K1
IC50
0.67 μM
Compound: B, SPL
Antagonist activity at human androgen receptor expressed in CHOK1 cells assessed as inhibition of D(-)-norgestrel-induced protein interaction with steroid receptor co-activator peptide after 24 hrs by beta-galactosidase reporter gene assay
Antagonist activity at human androgen receptor expressed in CHOK1 cells assessed as inhibition of D(-)-norgestrel-induced protein interaction with steroid receptor co-activator peptide after 24 hrs by beta-galactosidase reporter gene assay
Antagonist activity at mineralocorticoid receptor ligand binding domain expressed in african green monkey COS7 cells co-transfected with Gal4-LBD by luciferase reporter gene assay
Antagonist activity at mineralocorticoid receptor ligand binding domain expressed in african green monkey COS7 cells co-transfected with Gal4-LBD by luciferase reporter gene assay
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Inhibited the expression of monocyte chemoattractant protein-1 (MCP-1) and tumor necrosis factor-α (TNF-α).
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
Hypertensive transgenic mice that overproduce angiotensin II (AngII)[1]
Dosage:
20 mg/kg; Once day; 4 weeks
Administration:
i.h.
Result:
Eliminated intimal hyperplasia and medial hypertrophy, inhibited the expression of osteopontin (OPN), and had an inhibitory effect on AngII.
Increased mouse lifespan, did not significantly improve hypercalcemia, hyperphosphatemia or excess 1,25(OH)2D3 and FGF23 plasma concentrations, reduced tissue calcification in kl/kl mice, reduced PIT1, osteoblast differentiation Promoter for expression of Tnfa, Alpl, Msx2, Cbfa1, Osx.
Subcutaneous injection (s.c.) for Hot-plate assay, Tail electric stimulation test, Capsaicin-induced hind paw licking; Oral gavage (p.o.) for Acetic acid-induced writhing; i.p. for Rotarod testing
Result:
Reduced response latency in the hot plate test. Lowering the nociceptive threshold of electrically induced pain in mice. Caused significant anti-pain effects in acetic acid-induced writhing experiments in mice and reduced capsaicin-induced chemical pain at doses of 20-160 mg/kg. Reduced locomotor activity in mice and produced significant impairment in the rotation test at doses of 40 or 80 mg/kg.
Animal Model:
Leptin receptor knockout (db/db) mice, a model of DM2[4]
Dosage:
50 mg/kg , daily, 6 weeks
Administration:
Oral gavage (p.o.)
Result:
Eliminated endothelial dysfunction in the arteries of db/db mice, increased endothelial nitric oxide synthase (eNOS) phosphorylation (Ser1177), increased the expression of superoxide dismutase-1 and catalase in the arteries of db/db mice, improved relaxation induced by sodium nitroprusside and BAY 41-2277, and increased the expression of soluble corona yl cyclase (sGC) β subunit.
Decreased blood lipid and blood glucose levels, improved liver and kidney function, reduced urinary albumin excretion, restored podocyte morphology to relative normality, and autophagic vacuoles could be seen in podocytes.
Room temperature in continental US; may vary elsewhere.
Storage
Powder
-20°C
3 years
4°C
2 years
In solvent
-80°C
1 year
-20°C
6 months
Solvent & Solubility
In Vitro:
DMSO : ≥ 50 mg/mL (120.03 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
*"≥" means soluble, but saturation unknown.
Preparing Stock Solutions
ConcentrationSolventMass
1 mg
5 mg
10 mg
1 mM
2.4006 mL
12.0028 mL
24.0056 mL
5 mM
0.4801 mL
2.4006 mL
4.8011 mL
10 mM
0.2401 mL
1.2003 mL
2.4006 mL
View the Complete Stock Solution Preparation Table
*Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles. Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day. The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μLDMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.00 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μLDMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3
Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (6.00 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μLDMSO stock solution (25.0 mg/mL) to 900 μLCorn oil, and mix evenly.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
Dosage
mg/kg
Animal weight (per animal)
g
Dosing volume (per animal)
μL
Number of animals
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO+
%
+
%
Tween-80
+
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO,
. All of co-solvents are available by MedChemExpress (MCE).
, Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration:
mg/mL
Method for preparing stock solution:
mg
drug dissolved in
μL
DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take
μL DMSO stock solution, add
μL .
μL , mix evenly, next add
μL Tween 80, mix evenly, then add
μL Saline.
Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution
If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
*Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles. Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.
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