2. Metabolic Enzyme/Protease Vitamin D Related/Nuclear Receptor Immunology/Inflammation Apoptosis
  3. Mineralocorticoid Receptor Glucocorticoid Receptor Apoptosis
  4. Fludrocortisone

Fludrocortisone  (Synonyms: 9α-Fludrocortisone; 9α-Fluorcortisol)

Cat. No.: HY-B1203 Purity: 98.99%
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Fludrocortisone (9α-Fludrocortisone) is an orally active mineralocorticoid and glucocorticoid receptor agonist. Fludrocortisone suppresses pro-inflammatory cytokine expression, reduces CCL2, IL-6, IL-8 levels, upregulates mineralocorticoid receptor (MR) expression, induces PI3K/Akt, GSK-3β, CREB, ERK1/2, mTOR phosphorylation, blocks Tau hyperphosphorylation, prevents apoptosis, promotes survival and proliferation, enhances renal sodium and water transport, increases plasma volume and blood pressure, reduces plasma potassium and renin activity, stimulates erythropoietin expression, modulates uterine receptivity genes, and reverses PP242-induced MUC1 upregulation. Fludrocortisone can be used for the research of congenital adrenal hyperplasia, postural hypotension, and adrenal insufficiency.

For research use only. We do not sell to patients.

Fludrocortisone

Fludrocortisone Chemical Structure

CAS No. : 127-31-1

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10 mM * 1 mL in DMSO
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Fludrocortisone Related Antibodies

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Description

Fludrocortisone (9α-Fludrocortisone) is an orally active mineralocorticoid and glucocorticoid receptor agonist. Fludrocortisone suppresses pro-inflammatory cytokine expression, reduces CCL2, IL-6, IL-8 levels, upregulates mineralocorticoid receptor (MR) expression, induces PI3K/Akt, GSK-3β, CREB, ERK1/2, mTOR phosphorylation, blocks Tau hyperphosphorylation, prevents apoptosis, promotes survival and proliferation, enhances renal sodium and water transport, increases plasma volume and blood pressure, reduces plasma potassium and renin activity, stimulates erythropoietin expression, modulates uterine receptivity genes, and reverses PP242-induced MUC1 upregulation. Fludrocortisone can be used for the research of congenital adrenal hyperplasia, postural hypotension, and adrenal insufficiency[1][2][3][4][5][6].

In Vitro

Fludrocortisone (0.01-10 μg/μL; 12 h) is non-cytotoxic to MIO-M1, ARPE19, and 661W human retinal cell lines at concentrations up to 1 μg/μL, with reduced viability only seen at 10 μg/μL in MIO-M1 and 661W cells[1].
Fludrocortisone (1 μg/μL; 12 h) potently suppresses IL-1β- and TNF-α-induced CCL2, IL-6, and IL-8 mRNA expression in MIO-M1 human Müller glial cells[1].
Fludrocortisone (1 μM; 24 h) increases mineralocorticoid receptor
(MR) gene expression in AHPs without altering glucocorticoid receptor (GR) expression[2].
Fludrocortisone (0.5-2 μM; 24 h) promotes survival, proliferation, and reduces apoptosis in growth factor-deprived AHPs, with 1 μM being the optimal concentration[2].
Fludrocortisone (1 μM) activates cAMP/PKA/CREB signaling in AHPs, which is required for its pro-survival and pro-proliferative effects[2].
Fludrocortisone (1 μM) activates PI3K/Akt and mTOR/p70S6K signaling, and inactivates GSK-3β, which is required for its protective effects in growth factor-deprived AHPs[2].
Fludrocortisone (1 μM) protects AHPs from Aβ1-42-induced toxicity by promoting survival, proliferation, reducing apoptosis, restoring Akt/GSK-3β phosphorylation, and blocking Tau hyperphosphorylation[2].
Fludrocortisone (4-6 h) stimulates Epo, HIF2α, HIF1α, and PHD2 mRNA expression in microdissected rat nephron segments and mouse kidney nephron segments and peritubular cells, with significant increases relative to basal conditions[5].
Fludrocortisone (6 h, 72 h) significantly increases Epo protein expression in rat renal cortex but not in rat liver, relative to basal conditions[5].
Fludrocortisone (4-6 h) stimulates Epo protein production in mouse MAL, CCD, and OMCD, with specific upregulation in type A intercalated cells of the collecting ducts, and effects diminish to basal levels by 72 h[5].

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

Fludrocortisone Related Antibodies

Cell Viability Assay[1]

Cell Line: human MIO-M1 Müller glial cells, ARPE19 retinal pigment epithelial cells, 661W cone photoreceptor-like cells
Concentration: 0.01-10 μg/μL
Incubation Time: 12 h
Result: Did not significantly alter cell viability in ARPE19 cells at all tested concentrations. Showed unchanged viability in MIO-M1 and 661W cells at 0.01, 0.1, and 1 μg/μL; caused a slight but statistically significant reduction in viability only at the highest concentration of 10 μg/μL in MIO-M1 and 661W cells.

Real Time qPCR[1]

Cell Line: human MIO-M1 Müller glial cells
Concentration: 1 μg/μL
Incubation Time: 12 h (co-incubated with IL-1β stimulation)
Result: Completely abrogated IL-1β-induced significant increases in CCL2, IL-6, and IL-8 mRNA expression, suppressing expression to near baseline levels.

Real Time qPCR[1]

Cell Line: human MIO-M1 Müller glial cells
Concentration: 1 μg/μL
Incubation Time: 12 h (co-incubated with TNF-α stimulation)
Result: Sharply reduced TNF-α-induced significant increases in CCL2, IL-6, and IL-8 mRNA expression, suppressing expression to near baseline levels.

Real Time qPCR[1]

Cell Line: Human MIO-M1 Müller glial cells
Concentration: 1 μg/μL
Incubation Time: 12 h (co-incubated with IL-1β stimulation)
Result: Had its suppressive effect on IL-1β-induced CCL2, IL-6, and IL-8 expression completely abrogated by co-incubation with glucocorticoid receptor antagonist RU486.

Real Time qPCR[2]

Cell Line: Adult rat hippocampal progenitor cells (AHPs)
Concentration: 1 μM
Incubation Time: 24 h
Result: Strongly increased mineralocorticoid receptor (MR) gene expression; showed no significant change in glucocorticoid receptor (GR) gene expression.

Cell Viability Assay[2]

Cell Line: Adult rat hippocampal progenitor cells (AHPs)
Concentration: 0.01, 0.1, 0.5, 1, 2 μM
Incubation Time: 24 h
Result: Progressively increased cell survival and proliferation at 0.5, 1, and 2 μM; strongly reduced serum starvation-induced apoptosis (via decreased caspase-3 activity) at 0.5, 1, and 2 μM; identified 1 μM as the optimal concentration for subsequent experiments.

Western Blot Analysis[2]

Cell Line: adult rat hippocampal progenitor cells (AHPs)
Concentration: 1 μM (cAMP/CREB phosphorylation assays); 1 μM (functional validation with KT5720)
Incubation Time: 5, 15, 30, 60, 90 min (cAMP/CREB phosphorylation assays); 24 h (functional validation with KT5720)
Result: Increased intracellular cAMP levels, with a peak at 15 min and sustained elevation through 90 min; promoted CREB phosphorylation (Ser133), peaking at 15-30 min and returning to near basal levels by 90 min; had induced survival and proliferation reduced by co-treatment with PKA inhibitor KT5720.

Western Blot Analysis[2]

Cell Line: adult rat hippocampal progenitor cells (AHPs)
Concentration: 1 μM (phosphorylation assays); 1 μM (functional validation with wortmannin/rapamycin)
Incubation Time: 5, 15, 30, 60, 90 min (phosphorylation assays); 24 h (functional validation with wortmannin/rapamycin)
Result: Induced time-dependent phosphorylation of Akt (peaking at 30 min, sustained through 90 min), GSK-3β (sustained elevation from 5 to 90 min), and p70S6K (progressive elevation through 90 min); had induced survival, proliferation, and antiapoptotic effects reduced by co-treatment with Wortmannin or Rapamycin.
In Vivo

Fludrocortisone (1 μg/μL; intravitreal injection (3 μL); single dose) exerts neuroprotective effects in a mouse photo-oxidative retinal degeneration model, preserving retinal structure and function, reducing photoreceptor apoptosis, and inhibiting macrophage infiltration[1].
Fludrocortisone (1.5 mg/kg; i.p.; twice on Days 4 and 5 of pregnancy) modulates uterine receptivity in pregnant BALB/c mice by upregulating LIF, HB-EGF, Msx.1, and miRNA Let-7a, and activating the ERK1/2-mTOR pathway without altering MUC1 or miRNA 223-3p expression[4].
Fludrocortisone (1.5 mg/kg; i.p.; twice on Days 4 and 5 of pregnancy) co-administered with PP242 (30 mg/kg) reverses PP242-induced MUC1 upregulation and restores upregulation of key uterine receptivity genes (LIF, HB-EGF, Msx.1, miRNA Let-7a) in pregnant BALB/c mice[4].
Fludrocortisone (2.5 mg/100 g BW/day; i.p.; daily) stimulates renal Epo mRNA expression (peak at 4 hours) and Epo protein expression (at 6 and 72 hours) in male Sprague Dawley rats, with a statistically significant increase in plasma Epo concentration at 6 hours post-administration[5].

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

Animal Model: C57BL/6J (60 post-natal days old)[1]
Dosage: 1 μg/μL
Administration: intravitreal injection; single dose
Result: Preserved outer nuclear layer thickness at locations 1-2 mm and 2-3 mm superior to the optic nerve compared to controls; Achieved significantly higher a-wave and b-wave ERG responses; Reduced the number of TUNEL+ apoptotic photoreceptors significantly compared to vehicle-treated mice; Decreased the number of subretinal IBA1+ macrophages significantly compared to vehicle-treated mice.
Animal Model: BALB/c (8-week-old virgin female; pregnancy model, estrous induced, mated with fertile males, vaginal plug confirmed)[4]
Dosage: 1.5 mg/kg
Administration: i.p.; twice on Days 4 and 5 of pregnancy at 8:00 a.m.
Result: Did not significantly alter mRNA expression of mucin-1 (MUC1) or miRNA 223-3p; significantly upregulated mRNA expression of leukemia inhibitory factor (LIF), heparin-binding epidermal growth factor (HB-EGF, Msx.1, and miRNA Let-7a; significantly increased phosphorylated ERK1/2 (p-ERK1/2) and phosphorylated mammalian target of rapamycin (p-mTOR) levels; did not change phosphorylated eukaryotic translation initiation factor 4E-binding protein 1 (p-4E-BP1) levels significantly; induced round epithelial cell nuclei, cuboidal endometrial epithelium, no detectable glycoprotein layer on the epithelial surface, a thin continuous basement membrane beneath epithelial cells, and proliferating fibroblast-like stromal cells.
Animal Model: BALB/c (8-week-old virgin female; pregnancy model, estrous induced, mated with fertile males, vaginal plug confirmed)[4]
Dosage: 1.5 mg/kg (fludrocortisone); 30 mg/kg (PP242)
Administration: i.p.; twice on Days 4 and 5 of pregnancy at 8:00 a.m. (fludrocortisone); co-administered with PP242
Result: Significantly upregulated mRNA expression of LIF, HB-EGF, Msx.1, and miRNA Let-7a compared to PP242-only group; significantly downregulated mRNA expression of MUC1 compared to PP242-only group; did not change miRNA 223-3p expression significantly compared to PP242-only group.
Animal Model: Sprague Dawley (male)[5]
Dosage: 2.5 mg/100 g BW/day
Administration: i.p.; daily
Result: Increased Epo, HIF2α, and HIF1α mRNA expression in renal cortex at 4 hours post-injection; the stimulating effect disappeared by 72 hours. Increased Epo protein expression in renal cortex at 6 and 72 hours. Increased plasma Epo concentration at 6 hours (statistically significant elevation vs. vehicle), but not at 72 hours. Did not alter Epo mRNA or protein expression in the liver.
Clinical Trial
Molecular Weight

380.45

Formula

C21H29FO5
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

C[C@@]12[C@](C(CO)=O)(O)CC[C@@]1([H])[C@]3([H])CCC4=CC(CC[C@]4(C)[C@@]3(F)[C@@H](O)C2)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (262.85 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6285 mL 13.1423 mL 26.2847 mL
5 mM 0.5257 mL 2.6285 mL 5.2569 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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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    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (6.57 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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (6.57 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 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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: 98.99%

SDS (557 KB)

COA (252 KB) HNMR (320 KB) CNMR (278 KB) RP-HPLC (261 KB) LCMS (113 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.6285 mL 13.1423 mL 26.2847 mL 65.7117 mL
5 mM 0.5257 mL 2.6285 mL 5.2569 mL 13.1423 mL
10 mM 0.2628 mL 1.3142 mL 2.6285 mL 6.5712 mL
15 mM 0.1752 mL 0.8762 mL 1.7523 mL 4.3808 mL
20 mM 0.1314 mL 0.6571 mL 1.3142 mL 3.2856 mL
25 mM 0.1051 mL 0.5257 mL 1.0514 mL 2.6285 mL
30 mM 0.0876 mL 0.4381 mL 0.8762 mL 2.1904 mL
40 mM 0.0657 mL 0.3286 mL 0.6571 mL 1.6428 mL
50 mM 0.0526 mL 0.2628 mL 0.5257 mL 1.3142 mL
60 mM 0.0438 mL 0.2190 mL 0.4381 mL 1.0952 mL
80 mM 0.0329 mL 0.1643 mL 0.3286 mL 0.8214 mL
100 mM 0.0263 mL 0.1314 mL 0.2628 mL 0.6571 mL
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Fludrocortisone Related Classifications

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  • 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:

Fludrocortisone127-31-19α-Fludrocortisone 9α-FluorcortisolMineralocorticoid ReceptorGlucocorticoid ReceptorApoptosisCREBglucocorticoid receptormTORmineralocorticoid receptorGSK-3βERK1/2MIO-M1PI3K/AktARPE19aldosterone receptorInhibitorinhibitorinhibit

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