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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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Purity: ≥98%
Dexamethasone palmitate, the palmitate salt and a prodrug of Dexamethasone with anti-inflammatory and immunosuppressant activities, is a liposteroid for treatment of hemophagocytic lymphohistiocytosis. Dexamethasone palmitate (DXP) has 47-fold lower affinity for the glucocorticoid receptor than Dexamethasone.
| Targets |
Glucocorticoid receptor
|
|---|---|
| ln Vitro |
In RAW 264.7 cells, dexamethasone palmitate (100 μg/mL; 48 hours) alters the amounts of cytokines [1].
|
| ln Vivo |
Different distributions of dexamethasone palmitate (1280 μg; one IVT injection) are seen in ocular tissues at different periods [2]. Dexamethasone palmitate (280–1280 μg; after intravenous administration) modulates vascular hyperpermeability generated by VEGF [2].
|
| Cell Assay |
Cell viability assay [1]
Cell Types: RAW 264.7 Cell Tested Concentrations: 100 μg/mL Incubation Duration: 48 hrs (hours) Experimental Results: demonstrated in vitro anti-inflammatory effects and diminished LPS-induced MCP-1 and TNF-α concentrations in RAW 264.7 cells. |
| Animal Protocol |
Animal/Disease Models: New Zealand White Rabbit [2]
Doses: 1280 μg Route of Administration: IVT injection; 1280 μg Primary Experimental Results:Most of it is distributed in the vitreous body and still exists until 9 months. The distribution in the aqueous humor is minimal and almost disappears by 6 months. Animal/Disease Models: New Zealand white rabbits were injected with VEGF[2] Doses: 280, 560, 1280 μg Route of Administration: IVT injection; 280-1280 μg Primary Experimental Results: After 9 months of administration, VEGF-induced vascular permeability was controlled at Concentrations of 1280 μg, in addition to 280 and 560 μg also diminished VEGF-induced vascular hyperpermeability after 4 months of administration. |
| References |
[1]. Lorscheider M, et al. Dexamethasone palmitate nanoparticles: An efficient treatment for rheumatoid arthritis. J Control Release. 2019 Feb 28;296:179-189.
[2]. Daull P, 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 Mar;29(2):258-69. |
| Additional Infomation |
Dexamethasone palmitate is an organic molecular entity.
|
| Molecular Formula |
C38H58FO7
|
|---|---|
| Molecular Weight |
645.87
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| Exact Mass |
630.429
|
| Elemental Analysis |
C, 70.67; H, 9.05; F, 2.94; O, 17.34
|
| CAS # |
14899-36-6
|
| Related CAS # |
3936-02-5 (metasulfobenzoate sodium);3800-84-8 (sodium succinate);50-02-2;1177-87-3 (acetate); 150587-07-8 (beloxil); 132245-57-9 (cipecilate); 2265-64-7 (isonicotinate); 312-93-6 (phosphate); 2392-39-4 (sodium phosphate);
|
| PubChem CID |
63044
|
| Appearance |
Typically exists as white to off-white solids at room temperature
|
| Density |
1.1±0.1 g/cm3
|
| Boiling Point |
710.1±60.0 °C at 760 mmHg
|
| Melting Point |
60-65ºC
|
| Flash Point |
383.2±32.9 °C
|
| Vapour Pressure |
0.0±5.1 mmHg at 25°C
|
| Index of Refraction |
1.537
|
| LogP |
10.4
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
7
|
| Rotatable Bond Count |
18
|
| Heavy Atom Count |
45
|
| Complexity |
1130
|
| Defined Atom Stereocenter Count |
8
|
| SMILES |
CCCCCCCCCCCCCCCC(=O)OCC(=O)[C@]1([C@H](C)C[C@H]2[C@@H]3CCC4=CC(=O)C=C[C@]4(C)[C@]3([C@H](C[C@@]21C)O)F)O
|
| InChi Key |
QCUCMHCFYXPZII-YFWNWJEWSA-N
|
| InChi Code |
InChI=1S/C38H58FO7/c1-5-6-7-8-9-10-11-12-13-14-15-16-17-18-34(44)46-31-23-35(3)27(22-30(31)41)19-20-28-29-21-26(2)38(45,33(43)25-40)36(29,4)24-32(42)37(28,35)39/h22-23,25-26,28-29,32,40,42,45H,5-21,24H2,1-4H3/t26-,28+,29+,32+,35+,36+,37+,38+/m1/s1
|
| Chemical Name |
Palmitic acid, 21-ester with 9-fluoro-11beta,17,21-trihydroxy-16alpha-methylpregna-1,4-diene-3,20-dione
|
| Synonyms |
DXP; Limethason; Dexamethasone 21-palmitate; Dexamethasone 21-palmitate; Dexamethasone palmitate [JAN]; Limethason; 601XWN7060; [2-[(8S,9R,10S,11S,13S,14S,16R,17R)-9-fluoro-11,17-dihydroxy-10,13,16-trimethyl-3-oxo-6,7,8,11,12,14,15,16-octahydrocyclopenta[a]phenanthren-17-yl]-2-oxoethyl] hexadecanoate; Dexamethasone palmitate (JAN);
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~79.26 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.30 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.08 mg/mL (3.30 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (3.30 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.5483 mL | 7.7415 mL | 15.4830 mL | |
| 5 mM | 0.3097 mL | 1.5483 mL | 3.0966 mL | |
| 10 mM | 0.1548 mL | 0.7741 mL | 1.5483 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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