Dexamethasone palmitate

Synonyms: DXP

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. Dexamethasone palmitate (DXP) exhibits anti-inflammatory activity.

Dexamethasone palmitate Chemical Structure

Dexamethasone palmitate Chemical Structure

CAS No. 14899-36-6

Purity & Quality Control

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

Dexamethasone palmitate Related Products

Biological Activity

Description 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. Dexamethasone palmitate (DXP) exhibits anti-inflammatory activity.
Targets
Glucocorticoid receptor [1]
In vitro
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]

In Vivo
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]

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

Chemical Information & Solubility

Molecular Weight 630.87 Formula

C38H59FO6

CAS No. 14899-36-6 SDF --
Smiles CCCCCCCCCCCCCCCC(=O)OCC(=O)C1(O)C(C)CC2C3CCC4=CC(=O)C=CC4(C)C3(F)C(O)CC12C
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (158.51 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble


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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.

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