Dexamethasone palmitate (Synonyms: Dexamethasone 21-palmitate, DXP, Limethason) |
|
Catalog No.GC38573
|
Dexamethasone palmitate is a highly lipophilic glucocorticoid prodrug. Dexamethasone palmitate exhibits 47-fold lower affinity for the glucocorticoid receptor compared to Dexamethasone.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 14899-36-6
Sample solution is provided at 25 µL, 10mM.
Dexamethasone palmitate is a highly lipophilic glucocorticoid prodrug. Dexamethasone palmitate exhibits 47-fold lower affinity for the glucocorticoid receptor compared to Dexamethasone. Dexamethasone palmitate can be hydrolyzed by esterases in inflamed tissues to the active metabolite dexamethasone, exerting anti-inflammatory and immunosuppressive effects. Dexamethasone palmitate can inhibit macrophage chemotaxis, phagocytosis, and reactive oxygen species release. Dexamethasone palmitate can be used in related research on rheumatoid arthritis, graft-versus-host disease, macular edema, and sudden sensorineural hearing loss[1-4].
In vitro, treatment of macrophages activated with 100ng/mL LPS and 20ng/mL IFN-γ with 25μM Dexamethasone palmitate for 6-24 hours promoted rapid cell detachment from culture plates and reduced macrophage viability[5]. Treatment of RAW264.7 cells activated with 0.1μg/mL LPS with 100μg/mL Dexamethasone palmitate nanoparticles for 24 hours reduced TNF-α and MCP-1 secretion levels[6].
In vivo, intravitreal injection of 4μg Dexamethasone palmitate (0.5μL) immediately after laser-induced choroidal neovascularization in the right eye of Brown Norway rats. Dexamethasone palmitate reduced fluorescein leakage scores and decreased choroidal neovascularization volume[7]. Intravenous injection of 10mg/kg Dexamethasone palmitate on day 7 and day 14 after transplantation in C57BL/6J mice with lethal graft-versus-host disease (GVHD). Dexamethasone palmitate reduced clinical GVHD scores, decreased skin and intestinal tissue damage and F4/80⁺ macrophage numbers, and increased survival rate[8]. Inhalation of solid lipid nanoparticles containing Dexamethasone palmitate (5, 10, or 15mg/kg) via mesh nebulizer for 20 minutes in C57BL/6JNarl mice with intratracheal LPS-induced lung inflammation. Dexamethasone palmitate reduced TNF-α and IL-6 levels in bronchoalveolar lavage fluid, alleviated alveolar immune cell infiltration in lung tissue, and maintained alveolar and bronchiolar structural integrity[9].
References:
[1] Ahn JH. Dexamethasone palmitate: A promising intratympanic treatment option for severe sudden hearing loss. Am J Otolaryngol. 2026 Jan-Feb;47(1):104766.
[2] Wang B, Huang C, Xu L, et,al. Bioequivalence evaluation of dexamethasone palmitate injections by intravenous injection in healthy Chinese volunteers: a 2-period crossover trial. Naunyn Schmiedebergs Arch Pharmacol. 2025 Dec;398(12):17735-17743.
[3] Lei Y, Cao YX, Xu CB, et al. The Raf-1 inhibitor GW5074 and dexamethasone suppress sidestream smoke-induced airway hyperresponsiveness in mice. Respir Res. 2008 Nov 3;9:71.
[4]Ono R, Sakamoto K, Doi T, et al. Dexamethasone palmitate for children with Epstein-Barr virus associated hemophagocytic lymphohistiocytosis. Int J Hematol. 2025 Feb;121(2):252-256.
[5] Nishiwaki S, Nakayama T, Murata M, et al. Dexamethasone palmitate successfully attenuates hemophagocytic syndrome after allogeneic stem cell transplantation: macrophage-targeted steroid therapy. Int J Hematol. 2012 Apr;95(4):428-433.
[6] Lorscheider M, Tsapis N, ur-Rehman M, et al. Dexamethasone palmitate nanoparticles: An efficient treatment for rheumatoid arthritis. J Control Release. 2019 Apr 10;296:179-189.
[7] Daull P, Paterson CA, Kuppermann BD, et al. A preliminary evaluation of dexamethasone palmitate emulsion: a novel intravitreal sustained delivery of corticosteroid for treatment of macular edema. J Ocul Pharmacol Ther. 2013;29(2):258-269.
[8] Nishiwaki S, Nakayama T, Murata M, et al. Dexamethasone Palmitate Ameliorates Macrophages-Rich Graft-versus-Host Disease by Inhibiting Macrophage Functions. PLoS ONE. 2014 May 7;9(5):e96252.
[9] Chen H-H, Sang C-H, Chou C-W, et al. Solid Lipid Nanoparticles Loaded with Dexamethasone Palmitate for Pulmonary Inflammation Treatment by Nebulization Approach. Pharmaceutics. 2024 Jun;16(7):878.
| Cell experiment [1]: | |
|
Cell lines |
RAW 264.7 cells (mouse macrophage cell line) |
|
Preparation Method |
RAW 264.7 cells were seeded in 24-well plates at 4×104 cells/well and incubated 48h until 80% confluency. Cells were stimulated with 0.1μg/mL LPS for 3h, then treated with Dexamethasone palmitate nanoparticles at 100μg/mL (equivalent to 82μg/mL free dexamethasone phosphate) for 24h. Supernatants were collected and TNF-α and MCP-1 levels were quantified by cytometric beads array. |
|
Reaction Conditions |
100μg/mL; 24h |
|
Applications |
Dexamethasone palmitate nanoparticles reduced TNF-α secretion and MCP-1 secretion in LPS-activated RAW 264.7 macrophages. |
| Animal experiment [2]: | |
|
Animal models |
Lethally irradiated C57BL/6J mice (recipient) with BALB/c donor TCD-BM (5×106) and T lymphocytes (1×107) co-transplanted via tail vein |
|
Preparation Method |
Mice were intravenously administered 10mg/kg Dexamethasone palmitate on day 7 and day 14 after transplantation. Mice were monitored daily for clinical GVHD score (3 times/week until day 42), survival, and were sacrificed for histopathologic analysis of skin and gut, F4/80 immunohistochemistry, and FACS analysis of dermal macrophage chimerism. |
|
Dosage form |
10mg/kg; i.v.; twice does (day 7 and day 14) |
|
Applications |
Dexamethasone palmitate decreased clinical GVHD score, reduced skin and gut pathological GVHD scores, lowered F4/80⁺ macrophage number in skin and gut, reduced mRNA levels of TNF-α and IFN-γ and increased IL-10 in skin macrophages, and rescued about 20% of mice from GVHD-related death. |
References: [1] Lorscheider M, Tsapis N, ur-Rehman M, et al. Dexamethasone palmitate nanoparticles: An efficient treatment for rheumatoid arthritis. J Control Release. 2019 Apr 10;296:179-189. [2] Nishiwaki S, Nakayama T, Murata M, et al. Dexamethasone Palmitate Ameliorates Macrophages-Rich Graft-versus-Host Disease by Inhibiting Macrophage Functions. PLoS ONE. 2014 May 7;9(5):e96252. | |
| Cas No. | 14899-36-6 | SDF | |
| Synonyms | Dexamethasone 21-palmitate, DXP, Limethason | ||
| Canonical SMILES | C[C@@]12[C@](C[C@@H](C)[C@]2(O)C(COC(CCCCCCCCCCCCCCC)=O)=O)([H])[C@@]3([H])[C@@](F)([C@@]4(C(CC3)=CC(C=C4)=O)C)[C@@H](O)C1 | ||
| Formula | C38H59FO6 | M.Wt | 630.87 |
| Solubility | DMSO: 250 mg/mL (396.28 mM) | Storage | Store at -20°C |
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.5851 mL | 7.9256 mL | 15.8511 mL |
| 5 mM | 317 μL | 1.5851 mL | 3.1702 mL |
| 10 mM | 158.5 μL | 792.6 μL | 1.5851 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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.)
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 saline, 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.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 12 reference(s) in Google Scholar.)