Dexamethasone (MK-125)

Catalog No.S1322 Synonyms: NSC 34521, Hexadecadrol, Prednisolone F

For research use only.

Dexamethasone (MK-125, NSC 34521, Hexadecadrol, Prednisolone F) is a potent synthetic member of the glucocorticoid class of steroid drugs, and an interleukin receptor modulator that has anti-inflammatory and immunosuppressant effects. Dexamethasone induces autophagy and mitophagy. Dexamethasone is tested in hospitalized patients with COVID-19 and is found to have benefits for critically ill patients.

Dexamethasone (MK-125) Chemical Structure

CAS No. 50-02-2

Selleck's Dexamethasone (MK-125) has been cited by 56 publications

Purity & Quality Control

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Biological Activity

Description Dexamethasone (MK-125, NSC 34521, Hexadecadrol, Prednisolone F) is a potent synthetic member of the glucocorticoid class of steroid drugs, and an interleukin receptor modulator that has anti-inflammatory and immunosuppressant effects. Dexamethasone induces autophagy and mitophagy. Dexamethasone is tested in hospitalized patients with COVID-19 and is found to have benefits for critically ill patients.
Targets
interleukin receptor [1]
(Cell-free assay)
In vitro

Dexamethasone results in decrease in transmonolayer paracellular permeability mainly to sucrose, fluorescein and dextrans of up to 20 KDa in an immortalised rat brain endothelial cell line (GPNT). Dexamethasone results in filamentous actin and the cytoskeleton associated protein cortactin being highly concentrated in the regions of cell-cell contact with few F-actin stress fibres visible within the cytoplasm in cultured rat brain endothelial cells, an observation consistent with a more differentiated barrier phenotype induced by dexamethasone. Dexamethasone treatment has been shown to strongly stimulate the level of the Id-1 protein, which is a serum-inducible helix-loop-helix transcriptional repressor, involved in cell differentiation, and this effect was shown to be associated with reorganisation of ZO-1 to the cell periphery in Con8 mammary epithelial tumor cells. Dexamethasone prevents cytokine-induced enhanced expression of MMP-9 and alterations in the expression of ZO-1 in untreated GPNT monolayers. [1] Dexamethasone depletes both basal and TNF-alpha-stimulated GSH levels by down-regulating the gamma-GCS-heavy subunit transcription via a mechanism involving AP-1 (c-Jun) in alveolar epithelial cells. Dexamethasone decreases both basal and stimulated GSH levels (TNF-α-treated) in alveolar epithelial cells (A549), without any change in GSSG. [2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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Assay
Methods Test Index PMID
Western blot Bcl-2 / Bcl-xl / Mcl-1 / Survivin / IAP1 ; Cyclin D1 / Cyclin E / COX-2 / MMP-9 ; Bax / p21 ; p-JNK / JNK / p-p38 / p38 / p-ERK / ERK 28696369
In vivo Dexamethasone is administered i.m. to pregnant ewes, leads to the following results (1) blood pressure is unchanged; (2) as previously reported in the fetus, sensitivity to endothelin-1 (ET) is increased; (3) acetylcholine-induced relaxation is increased; (4) L-NAME suppressible vasodilatory response to ET is abolished; (5) there is no change in endothelium-independent vasodilatation; and (6) there is no change in eNOS RNA and protein levels, when compared to saline treated controls. [3]

Protocol (from reference)

Solubility (25°C)

In vitro

DMSO 79 mg/mL
(201.29 mM)
Water Insoluble
Ethanol '''6 mg/mL

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
5% DMSO+45% PEG 300+H2O
For best results, use promptly after mixing.

13mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 392.46
Formula

C22H29FO5

CAS No. 50-02-2
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1CC2C3CCC4=CC(=O)C=CC4(C3(C(CC2(C1(C(=O)CO)O)C)O)F)C

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05142098 Not yet recruiting Drug: Dexamethasone|Drug: Etoricoxib 60 mg Effect of Drug Dow University of Health Sciences January 1 2022 Early Phase 1
NCT05170789 Not yet recruiting Drug: Elotuzumab Selinexor and Dexamethasone (ESd) Relapsed Multiple Myeloma|Refractory Multiple Myeloma Tulane University School of Medicine|Karyopharm Therapeutics Inc|Tulane University January 7 2022 Phase 2
NCT05136781 Recruiting -- Thoracic Surgery|Anesthesiology|Corticosteroids|Respiratory Complication Centre Hospitalier Universitaire Amiens November 16 2021 --

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
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Frequently Asked Questions

Question 1:
I'm loonkig for Dexamethasone to use in cell culture, would it be better to use the Dexamethasone S1322, the sodiume phosphate S4028 or the acetate S3124?

Answer:
S1322 is the free base form of Dexamethasone, S4028 is the sodium phosphate form and S3124 is the acetate salt. All of them have similar biological activity in tissue culture, however, their suitabilities vary in different solvents. As free base, S1322 has high solubility in DMSO (79mg/ml), poor solubility in water (<1mg/ml), and moderate solubility in ethanol (6mg/ml). As sodium phosphate salt, S4028 has high solubility in water (103mg/ml) but is insoluble in DMSO and ethanol (<1mg/ml). The solubility of S3124 is 87mg/ml in DMSO, <1mg/ml in water, and 20mg/ml in ethanol. Selection can be made based on the customer's experimental setup.

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