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

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 (Ang II)-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.

CAS No. : 52-01-7

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Customer Review

Based on 7 publication(s) in Google Scholar

Other Forms of Spironolactone:

Spironolactone Related Antibodies

Top Publications Citing Use of Products

    Spironolactone purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Aug 23:e03409.  [Abstract]

    The MR inhibitor Spironolactone (Spir) (50 ng) significantly decreased the average CPA scores and inhibited CTR-MWM.

    Spironolactone purchased from MedChemExpress. Usage Cited in: Gene Rep. 2025 Oct 4.

    Spironolactone (20 mg/kg; i.g.; once daily for 4 weeks) significantly increased the expression levels of GAS6 AXL, and MR in mice with aldosterone-induced renal injury.

    Spironolactone purchased from MedChemExpress. Usage Cited in: Gene Rep. 2025 Oct 4.

    Treatment with MR antagonists Spironolactone (20 mg/kg; i.g.; once daily for 4 weeks) significantly reduced urinary protein (PRO) and urinary creatinine (UCR) levels.

    Spironolactone purchased from MedChemExpress. Usage Cited in: J Orthop Surg Res. 2024 Feb 19;19(1):147.  [Abstract]

    In vitro, Spironolactone (5 mg/kg; i.p.; every other day) significantly inhibited the proliferation ability of MCA-205.

    Spironolactone purchased from MedChemExpress. Usage Cited in: J Orthop Surg Res. 2024 Feb 19;19(1):147.  [Abstract]

    Spironolactone (5 mg/kg; i.p.; every other day) increased the amounts of VEGF of MCA-205 in the supernatant.

    View All Calcium Channel Isoform Specific Products:

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    • 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 (Ang II)-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
    		[PMID: 25941555]
    COS-1 IC50
    60 nM
    Compound: Spironolactone
    Antagonist activity at human MR transfected in human COS1 cells after 1 day by luciferase reporter gene assay
    Antagonist activity at human MR transfected in human COS1 cells after 1 day by luciferase reporter gene assay
    		[PMID: 22074142]
    COS-1 IC50
    60 nM
    Compound: Spironolactone
    Antagonist activity at human mineralocorticoid receptor expressed in COS1 cells after 1 day by luciferase reporter gene assay
    Antagonist activity at human mineralocorticoid receptor expressed in COS1 cells after 1 day by luciferase reporter gene assay
    		[PMID: 25187277]
    COS-7 IC50
    1.6 nM
    Compound: Spironolactone
    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
    		[PMID: 19863083]
    HEK293 IC50
    18.6 μM
    Compound: spironolactone
    Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay
    Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay
    		[PMID: 23241029]
    HEK293 IC50
    49 nM
    Compound: Spironolactone
    Displacement of [3H]aldosterone from cytosolic human MR expressed in HEK293 cells after 16 hrs by scintillation counting
    Displacement of [3H]aldosterone from cytosolic human MR expressed in HEK293 cells after 16 hrs by scintillation counting
    		[PMID: 22074142]
    Huh-7 IC50
    13 nM
    Compound: spironolactone
    Antagonist activity at Gal4-tagged mineralocorticoid receptor expressed in human Huh7 cells by luciferase reporter gene assay
    Antagonist activity at Gal4-tagged mineralocorticoid receptor expressed in human Huh7 cells by luciferase reporter gene assay
    		[PMID: 20672822]
    NIH-3T3-G185 IC50
    23.6 μM
    Compound: Spironolactone
    TP_TRANSPORTER: inhibition of Daunorubicin efflux in NIH-3T3-G185 cells
    TP_TRANSPORTER: inhibition of Daunorubicin efflux in NIH-3T3-G185 cells
    		[PMID: 11743742]
    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 Ang II-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.

    Spironolactone Related Antibodies

    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.
    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.

    • Molarity Calculator

    • 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
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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: 99.81%

    SDS (418 KB)

    COA (257 KB) HNMR (271 KB) RP-HPLC (259 KB) MS (68 KB)

    Handling Instructions (2659 KB)
    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 Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      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.

    Keywords:

    Spironolactone52-01-7SC9420SC 9420SC-9420Mineralocorticoid ReceptorAndrogen ReceptorAutophagyCalcium ChannelCa2+ channelsCa channelsOralPodocytesSelectiveDiabeticNephropathyAldosterone antagonistAnti-inflammatory effectsPain modulationVascular and soft tissue calcificationAntihypertensiveInhibitorinhibitorinhibit

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