1. Metabolic Enzyme/Protease Vitamin D Related/Nuclear Receptor Autophagy Membrane Transporter/Ion Channel Neuronal Signaling
  2. Mineralocorticoid Receptor Androgen Receptor Autophagy Calcium Channel
  3. Spironolactone

Spironolactone  (Synonyms: SC9420)

Cat. No.: HY-B0561 Purity: 99.66%
COA Handling Instructions

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.

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Spironolactone Chemical Structure

Spironolactone Chemical Structure

CAS No. : 52-01-7

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
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Solution
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Customer Review

Based on 3 publication(s) in Google Scholar

Other Forms of Spironolactone:

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

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[1][2][3][4][5][6][7][8][9][10].

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Real Time qPCR[2]

Cell Line: HAoSMCs (induced by 100 nM aldosterone)
Concentration: 10 μM
Incubation Time: 24 h
Result: Inhibited the mRNA expression of PITI, TNFA, MSX2, CBFA1 and ALPL.

Western Blot Analysis[5]

Cell Line: Angiotensin II-induced hu-PBMC
Concentration: 0, 100 nM, 1 µM, 10 µM
Incubation Time: 30 min
Result: 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.
Animal Model: Klotho-hypomorphic mice (kl/kl mice)[2]
Dosage: 80 mg/L
Administration: Oral gavage (p.o.)
Result: 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.
Animal Model: Male Swiss albino mice[3]
Dosage: 10, 20, 40 or 80 mg/kg
Administration: 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.
Animal Model: SD rat diabetic nephropathy (DN) model[10]
Dosage: 40mg/kg, daily, 8weeks
Administration: i.g.
Result: 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.
Clinical Trial
Molecular Weight

416.57

Formula

C24H32O4S

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

C[C@@]12[C@](OC3=O)(CC3)CC[C@@]1([H])[C@@]([C@@H](CC4=CC5=O)SC(C)=O)([H])[C@]([C@]4(CC5)C)([H])CC2

Shipping

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
Concentration Solvent Mass 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
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.

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  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

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.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% 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 μL DMSO 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 μL DMSO 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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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.
 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.
Purity & Documentation

Purity: 99.66%

References

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.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.4006 mL 12.0028 mL 24.0056 mL 60.0139 mL
5 mM 0.4801 mL 2.4006 mL 4.8011 mL 12.0028 mL
10 mM 0.2401 mL 1.2003 mL 2.4006 mL 6.0014 mL
15 mM 0.1600 mL 0.8002 mL 1.6004 mL 4.0009 mL
20 mM 0.1200 mL 0.6001 mL 1.2003 mL 3.0007 mL
25 mM 0.0960 mL 0.4801 mL 0.9602 mL 2.4006 mL
30 mM 0.0800 mL 0.4001 mL 0.8002 mL 2.0005 mL
40 mM 0.0600 mL 0.3001 mL 0.6001 mL 1.5003 mL
50 mM 0.0480 mL 0.2401 mL 0.4801 mL 1.2003 mL
60 mM 0.0400 mL 0.2000 mL 0.4001 mL 1.0002 mL
80 mM 0.0300 mL 0.1500 mL 0.3001 mL 0.7502 mL
100 mM 0.0240 mL 0.1200 mL 0.2401 mL 0.6001 mL
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Spironolactone
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