Home Endocrinology & Hormones Glucocorticoid Receptor agonist Dexamethasone palmitate

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Dexamethasone palmitate Glucocorticoid Receptor agonist

Cat.No.S5184

Dexamethasone palmitate (DXP), a lipophilic prodrug of Dexamethasone (DXM), is a glucocorticoid receptor agonist with a 47-fold lower affinity for the glucocorticoid receptor than DXM. This compound exhibits anti-inflammatory activity.
Dexamethasone palmitate Glucocorticoid Receptor agonist Chemical Structure

Chemical Structure

Molecular Weight: 630.87

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Quality Control

Batch: S518401 DMSO]100 mg/mL]false]Ethanol]100 mg/mL]false]Water]Insoluble]false Purity: 99.46%
99.46

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (158.51 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble

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In vivo
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Chemical Information, Storage & Stability

Molecular Weight 630.87 Formula

C38H59FO6

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 14899-36-6 -- Storage of Stock Solutions

Synonyms DXP Smiles CCCCCCCCCCCCCCCC(=O)OCC(=O)C1(O)C(C)CC2C3CCC4=CC(=O)C=CC4(C)C3(F)C(O)CC12C

Mechanism of Action

Targets/IC50/Ki
Glucocorticoid receptor
In vitro

Dexamethasone palmitate 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). This compound 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 this chemical. This compound 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. This chemical prevents cytokine-induced enhanced expression of MMP-9 and alterations in the expression of ZO-1 in untreated GPNT monolayers.  It 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. This compound decreases both basal and stimulated GSH levels (TNF-α-treated) in alveolar epithelial cells (A549), without any change in GSSG. 
In vivo

Dexamethasone palmitate 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. 
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/16166452/
  • [5] https://pubmed.ncbi.nlm.nih.gov/17440100/
  • [6] https://pubmed.ncbi.nlm.nih.gov/3877041/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04669262 Completed
Healthy
BeiGene
 December 9 2020 Phase 1
NCT04551898 Completed
Covid19
BeiGene
 December 2 2020 Phase 2
NCT04532294 Completed
Covid19
BeiGene
 September 8 2020 Phase 1

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