1. Immunology/Inflammation Vitamin D Related/Nuclear Receptor Metabolic Enzyme/Protease
  2. Glucocorticoid Receptor Endogenous Metabolite
  3. Prednisolone

Prednisolone is a potent, orally active corticosteroid and a glucocorticoid. Prednisolone possesses about four times the anti-inflammatory activity of hydrocortisone while causing less salt and water retention. Prednisolone can be used for ocular, anti-inflammatory research.

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

Prednisolone Chemical Structure

Prednisolone Chemical Structure

CAS No. : 50-24-8

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Customer Review

Based on 5 publication(s) in Google Scholar

Other Forms of Prednisolone:

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  • Biological Activity

  • Purity & Documentation

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Description

Prednisolone is a potent, orally active corticosteroid and a glucocorticoid. Prednisolone possesses about four times the anti-inflammatory activity of hydrocortisone while causing less salt and water retention. Prednisolone can be used for ocular, anti-inflammatory research[1][2].

Cellular Effect
Cell Line Type Value Description References
A549 EC50
0.002 nM
Compound: 2, pred
Agonist activity at human mineralocorticoid receptor expressed in human A549 cells by fluorescence polarization assay
Agonist activity at human mineralocorticoid receptor expressed in human A549 cells by fluorescence polarization assay
[PMID: 21899328]
A549 EC50
13.6 nM
Compound: 2, pred
Transrepression activity of glucocorticoid receptor in human A549 cells assessed as inhibition of IL1beta-stimulated NFkappaB-dependent E-selectin transcription by luciferase reporter gene assay
Transrepression activity of glucocorticoid receptor in human A549 cells assessed as inhibition of IL1beta-stimulated NFkappaB-dependent E-selectin transcription by luciferase reporter gene assay
[PMID: 21073190]
A549 EC50
13.6 nM
Compound: pred
Transrepression activity at GR in IL-1-beta-stimulated human A549 cells assessed as inhibition of NF-kappaB-dependent E-selectin transcription by luciferase reporter gene assay
Transrepression activity at GR in IL-1-beta-stimulated human A549 cells assessed as inhibition of NF-kappaB-dependent E-selectin transcription by luciferase reporter gene assay
[PMID: 19321341]
A549 EC50
14.4 nM
Compound: 2, pred
Transrepression activity at glucocorticoid receptor alpha in IL-1beta-stimulated human A549 cells assessed as inhibition of NFkappaB-dependent E-selectin transcription by luciferase reporter gene assay
Transrepression activity at glucocorticoid receptor alpha in IL-1beta-stimulated human A549 cells assessed as inhibition of NFkappaB-dependent E-selectin transcription by luciferase reporter gene assay
[PMID: 21899328]
A549 EC50
15.8 nM
Compound: 2, pred
Transrepression activity of glucocorticoid receptor in human A549 cells expressing AP-1 assessed as inhibition of PMA-induced AP-1 activity by luciferase reporter gene assay
Transrepression activity of glucocorticoid receptor in human A549 cells expressing AP-1 assessed as inhibition of PMA-induced AP-1 activity by luciferase reporter gene assay
[PMID: 21073190]
A549 EC50
16.1 nM
Compound: 2, pred
Transrepression activity at glucocorticoid receptor alpha in phorbol myristate acetate-stimulated human A549 cells assessed as inhibition of AP1 response element by luciferase reporter gene assay
Transrepression activity at glucocorticoid receptor alpha in phorbol myristate acetate-stimulated human A549 cells assessed as inhibition of AP1 response element by luciferase reporter gene assay
[PMID: 21899328]
A549 IC50
5.8 nM
Compound: Prednisolone
Antiinflammatory activity in human A549 cells assessed as inhibition of IL1beta-induced IL6 production preincubated for 30 mins followed by IL1beta-stimulation and measured after 20 hrs by AlphaLisa assay
Antiinflammatory activity in human A549 cells assessed as inhibition of IL1beta-induced IL6 production preincubated for 30 mins followed by IL1beta-stimulation and measured after 20 hrs by AlphaLisa assay
[PMID: 30384041]
C2C12 EC50
3.4 nM
Compound: Prednisolone
Inhibition of mouse glutamine synthetase by GR-mediated transactivation in C2C12 cells
Inhibition of mouse glutamine synthetase by GR-mediated transactivation in C2C12 cells
[PMID: 15808489]
CV-1 ED50
4 nM
Compound: prednisolone
Activity at human glucocorticoid receptor expressed in CV1 cells assessed as repression of TNF and IL-1-beta-induced E-selectin gene expression by luciferase reporter gene assay
Activity at human glucocorticoid receptor expressed in CV1 cells assessed as repression of TNF and IL-1-beta-induced E-selectin gene expression by luciferase reporter gene assay
[PMID: 18032610]
HeLa EC50
16 nM
Compound: 1b
Activation of MMTV in HeLa cells measured by luciferase activity
Activation of MMTV in HeLa cells measured by luciferase activity
[PMID: 17181172]
HeLa EC50
21 nM
Compound: 2, pred
Transactivation activity at GR-alpha in human NP1 Hela cells assessed as inhibition of GAL4-DBD after 20 hrs by luciferase reporter gene assay
Transactivation activity at GR-alpha in human NP1 Hela cells assessed as inhibition of GAL4-DBD after 20 hrs by luciferase reporter gene assay
[PMID: 21899328]
HeLa EC50
73.9 nM
Compound: 2, pred
Transactivation activity at GR-alpha in human NP1 Hela cells assessed as induction of GAL4-DBD after 20 hrs by luciferase reporter gene assay
Transactivation activity at GR-alpha in human NP1 Hela cells assessed as induction of GAL4-DBD after 20 hrs by luciferase reporter gene assay
[PMID: 21899328]
HeLa EC50
82.7 nM
Compound: 2, pred
Transactivation activity of glucocorticoid receptor ligand binding domain expressed in human NP-1 Hela cells co-expressing GAL4 DNA binding domain by luciferase reporter gene assay
Transactivation activity of glucocorticoid receptor ligand binding domain expressed in human NP-1 Hela cells co-expressing GAL4 DNA binding domain by luciferase reporter gene assay
[PMID: 21073190]
HepG2 IC50
23 nM
Compound: 1
Transrepression activity at glucocorticoid receptor in IL-1beta-stimulated human HepG2 cells assessed as inhibition of AP1 response element-induced IL-6 production by ELISA
Transrepression activity at glucocorticoid receptor in IL-1beta-stimulated human HepG2 cells assessed as inhibition of AP1 response element-induced IL-6 production by ELISA
[PMID: 21115247]
HepG2 EC50
26 nM
Compound: 1
Agonist activity at glucocorticoid receptor in human HepG2 cells co-transfected with PEPCK assessed as GRE activation by luciferase reporter gene assay
Agonist activity at glucocorticoid receptor in human HepG2 cells co-transfected with PEPCK assessed as GRE activation by luciferase reporter gene assay
[PMID: 21324689]
HepG2 IC50
4.1 nM
Compound: 1
Transrepression activity at GR expressed in IL-1beta- and TNFalpha-stimulated HepG2 cells assessed as inhibition of NFKB- or AP-1 mediated E-selectin transcription by luciferase reporter gene assay
Transrepression activity at GR expressed in IL-1beta- and TNFalpha-stimulated HepG2 cells assessed as inhibition of NFKB- or AP-1 mediated E-selectin transcription by luciferase reporter gene assay
[PMID: 21349714]
HepG2 IC50
4.1 nM
Compound: 1
Transrepression activity at glucocorticoid receptor in human HepG2 cells assessed as inhibition of TNFalpha/IL1beta-stimulated NFkappaB-dependent E-selectin repression by luciferase reporter gene assay
Transrepression activity at glucocorticoid receptor in human HepG2 cells assessed as inhibition of TNFalpha/IL1beta-stimulated NFkappaB-dependent E-selectin repression by luciferase reporter gene assay
[PMID: 21324689]
HepG2 IC50
4.1 nM
Compound: 1
Agonist activity at GR expressed in IL-1beta- and TNFalpha-stimulated HepG2 cells assessed as inhibition of NFKB- or AP-1 mediated E-selectin transcription by luciferase reporter gene assay relative to Dexamethasone
Agonist activity at GR expressed in IL-1beta- and TNFalpha-stimulated HepG2 cells assessed as inhibition of NFKB- or AP-1 mediated E-selectin transcription by luciferase reporter gene assay relative to Dexamethasone
[PMID: 21316964]
HepG2 IC50
4.1 nM
Compound: 1
Transrepression activity at glucocorticoid receptor in TNFalpha/IL1beta-stimulated human HepG2 cells assessed as inhibition of NFkappaB-dependent E-selectin transcription by luciferase reporter gene assay
Transrepression activity at glucocorticoid receptor in TNFalpha/IL1beta-stimulated human HepG2 cells assessed as inhibition of NFkappaB-dependent E-selectin transcription by luciferase reporter gene assay
[PMID: 21115247]
HepG2 EC50
5.3 nM
Compound: 1
Agonist activity at glucocorticoid receptor in human HepG2 cells co-transfected with GRE assessed as GRE activation by luciferase reporter gene assay
Agonist activity at glucocorticoid receptor in human HepG2 cells co-transfected with GRE assessed as GRE activation by luciferase reporter gene assay
[PMID: 21324689]
HepG2 EC50
5.3 nM
Compound: 1
Agonist activity at glucocorticoid receptor in human HepG2 cells co-transfected with GRE assessed as transactivation activity by luciferase reporter gene assay
Agonist activity at glucocorticoid receptor in human HepG2 cells co-transfected with GRE assessed as transactivation activity by luciferase reporter gene assay
[PMID: 21115247]
HFF EC50
19 nM
Compound: 1b
Induction of aromatase activity in HFF cells assessed as production of beta estradiol by aromatase assay
Induction of aromatase activity in HFF cells assessed as production of beta estradiol by aromatase assay
[PMID: 17181172]
Huh-7 EC50
57.4 nM
Compound: 2, pred
Transactivation activity at glucocorticoid receptor in human 13D3/Huh7 cells assessed as induction of tyrosine aminotransferase activity after 24 hrs
Transactivation activity at glucocorticoid receptor in human 13D3/Huh7 cells assessed as induction of tyrosine aminotransferase activity after 24 hrs
[PMID: 21073190]
Huh-7 EC50
64 nM
Compound: 2, pred
Transactivation activity at glucocorticoid receptor alpha human 13D3/Huh7 cells assessed as induction of TAT activity after 4 hrs by spectrophotometry
Transactivation activity at glucocorticoid receptor alpha human 13D3/Huh7 cells assessed as induction of TAT activity after 4 hrs by spectrophotometry
[PMID: 21899328]
L1210 ED50
100 μM
Compound: Prednisolone
Cytotoxicity against mouse L1210 cells assessed as growth inhibition measured at 72 hrs by trypan blue exclusion assay
Cytotoxicity against mouse L1210 cells assessed as growth inhibition measured at 72 hrs by trypan blue exclusion assay
[PMID: 118258]
MG-63 EC50
19 nM
Compound: 2, pred
Induction of glutamine synthase expression in human MG63 cells after overnight incubation by spectrophotometry
Induction of glutamine synthase expression in human MG63 cells after overnight incubation by spectrophotometry
[PMID: 21899328]
NHDF IC50
23 nM
Compound: 1
Transrepression activity at GR expressed in NHDF cells assessed as IL-1beta-mediated IL-6 transcription by ELISA
Transrepression activity at GR expressed in NHDF cells assessed as IL-1beta-mediated IL-6 transcription by ELISA
[PMID: 21349714]
NHDF IC50
23 nM
Compound: 1
Transrepression activity at glucocorticoid receptor in human NHDF cells assessed as inhibition of IL-1beta-stimulated AP1 dependent IL-6 repression by ELISA
Transrepression activity at glucocorticoid receptor in human NHDF cells assessed as inhibition of IL-1beta-stimulated AP1 dependent IL-6 repression by ELISA
[PMID: 21324689]
NHDF IC50
23 nM
Compound: 1
Agonist activity at human GR expressed in NHDF cells assessed as inhibition of IL-6 production by ELISA relative to Dexamethasone
Agonist activity at human GR expressed in NHDF cells assessed as inhibition of IL-6 production by ELISA relative to Dexamethasone
[PMID: 21316964]
OVCAR-3 IC50
1.1 μM
Compound: 35
Cytotoxicity against human OVCAR-3 cells incubated for 72 hrs by SRB assay
Cytotoxicity against human OVCAR-3 cells incubated for 72 hrs by SRB assay
[PMID: 32283298]
OVCAR-4 IC50
1.1 μM
Compound: 35
Cytotoxicity against human OVCAR-4 cells incubated for 72 hrs by SRB assay
Cytotoxicity against human OVCAR-4 cells incubated for 72 hrs by SRB assay
[PMID: 32283298]
PBMC IC50
13 nM
Compound: Pred
Antiinflammatory activity in Wistar rat PBMC assessed as inhibition of LPS-induced TNFalpha release preincubated for 45 mins followed by LPS addition after 18 hrs by ELISA
Antiinflammatory activity in Wistar rat PBMC assessed as inhibition of LPS-induced TNFalpha release preincubated for 45 mins followed by LPS addition after 18 hrs by ELISA
[PMID: 27810243]
PBMC IC50
45 nM
Compound: Pred
Antiinflammatory activity in human primary PBMC assessed as inhibition of LPS-induced TNFalpha release preincubated for 45 mins followed by LPS addition after 18 hrs by ELISA
Antiinflammatory activity in human primary PBMC assessed as inhibition of LPS-induced TNFalpha release preincubated for 45 mins followed by LPS addition after 18 hrs by ELISA
[PMID: 27810243]
RAW264.7 IC50
25.4 μM
Compound: Prednisolone
Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-induced TNFalpha production after 4 hrs by ELISA
Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-induced TNFalpha production after 4 hrs by ELISA
[PMID: 11000020]
T47D IC50
> 1000 nM
Compound: Prednisolone
Displacement of [3H]progesterone from progesterone receptor in human T47D cells after 20 hrs by scintillation counting method
Displacement of [3H]progesterone from progesterone receptor in human T47D cells after 20 hrs by scintillation counting method
[PMID: 30384041]
U-937 IC50
0.033 μM
Compound: Prednisolone
Antiinflammatory activity in human U937 cells assessed as inhibition of PMA/LPS-stimulated TNFalpha production after 24 hrs by ELISA
Antiinflammatory activity in human U937 cells assessed as inhibition of PMA/LPS-stimulated TNFalpha production after 24 hrs by ELISA
[PMID: 32631542]
U-937 IC50
0.44 μM
Compound: Prednisolone
Inhibition of LPS-induced IL-1beta expression in human U-937 cells preincubated for 1 hr followed by LPS addition and measured after 24 hrs by ELISA
Inhibition of LPS-induced IL-1beta expression in human U-937 cells preincubated for 1 hr followed by LPS addition and measured after 24 hrs by ELISA
[PMID: 31883489]
U-937 IC50
0.64 μM
Compound: Prednisolone
Inhibition of LPS-induced TNF-alpha expression in human U-937 cells preincubated for 1 hr followed by LPS addition and measured after 24 hrs by ELISA
Inhibition of LPS-induced TNF-alpha expression in human U-937 cells preincubated for 1 hr followed by LPS addition and measured after 24 hrs by ELISA
[PMID: 31883489]
U-937 IC50
8.2 nM
Compound: pred
Antiinflammatory activity in PMA-differentiated human U937 cells assessed as inhibition of LPS-induced TNFalpha production incubated for 60 mins prior to LPS challenge measured after 24 hrs
Antiinflammatory activity in PMA-differentiated human U937 cells assessed as inhibition of LPS-induced TNFalpha production incubated for 60 mins prior to LPS challenge measured after 24 hrs
[PMID: 24446728]
In Vitro

Prednisolone (0.002-10 μg/mL; 3 days) inhibits human leukocyte mitosis[4].

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

In Vivo

Prednisolone (5 mg/kg/day; p.o.; 6 days a week for 72 weeks) significantly prevents deaths from renal disease in mice[3].

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

Animal Model: NZB/NZW mice, immune nephritis model[3]
Dosage: 5 mg/kg/day
Administration: Oral, 6 days a week for 72 weeks
Result: Significantly lowered mortality rate and prolonged life significantly.
Clinical Trial
Molecular Weight

360.44

Formula

C21H28O5

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

C[C@@]1([C@@]2(O)C(CO)=O)[C@](CC2)([H])[C@@](CCC3=CC4=O)([H])[C@]([C@]3(C=C4)C)([H])[C@@H](O)C1

Structure Classification
Initial Source
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 : 62.5 mg/mL (173.40 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 0.1 mg/mL (0.28 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7744 mL 13.8719 mL 27.7439 mL
5 mM 0.5549 mL 2.7744 mL 5.5488 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.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

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

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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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: ≥ 2.08 mg/mL (5.77 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (5.77 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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:

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.
 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: 99.96%

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 2.7744 mL 13.8719 mL 27.7439 mL 69.3597 mL
5 mM 0.5549 mL 2.7744 mL 5.5488 mL 13.8719 mL
10 mM 0.2774 mL 1.3872 mL 2.7744 mL 6.9360 mL
15 mM 0.1850 mL 0.9248 mL 1.8496 mL 4.6240 mL
20 mM 0.1387 mL 0.6936 mL 1.3872 mL 3.4680 mL
25 mM 0.1110 mL 0.5549 mL 1.1098 mL 2.7744 mL
30 mM 0.0925 mL 0.4624 mL 0.9248 mL 2.3120 mL
40 mM 0.0694 mL 0.3468 mL 0.6936 mL 1.7340 mL
50 mM 0.0555 mL 0.2774 mL 0.5549 mL 1.3872 mL
60 mM 0.0462 mL 0.2312 mL 0.4624 mL 1.1560 mL
80 mM 0.0347 mL 0.1734 mL 0.3468 mL 0.8670 mL
100 mM 0.0277 mL 0.1387 mL 0.2774 mL 0.6936 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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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.

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Prednisolone
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