| Size | Price | Stock | Qty |
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| 250mg |
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| 500mg |
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| 1g |
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| Other Sizes |
Purity: ≥98%
| Targets |
Glucocorticoid receptor (likely mediates transcriptional regulation of tight junction proteins; no IC50/Ki/EC50/DC50 values reported). [1]
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| ln Vitro |
Dexamethasone inhibits COX-2 mRNA expression induced by IL-1 in human articular chondrocytes. Dexamethasone suppresses the cyclooxygenase-2 induction by tumor necrosis factor α (TNFα) with an IC50 of 1 nM in MC3T3-E1 cells. Dexamethasone binds to the glucocorticoid receptor and then to the glucocorticoid response element. Dexamethasone (10 μM) induces osteoblastic differentiation of rat bone marrow stromal cell cultures with elevated mRNA expression of alkaline phosphatase osteopontin, bone sialoprotein, and osteocalcin. Dexamethasone (5 μM) treatment decreases proliferation of adult hippocampal neural progenitor cells and SRE-driven gene expression.
Treatment of GPNT cells with 1 μM Dexamethasone Sodium Phosphate (as dexamethasone) from seeding decreased paracellular permeability to [14C]sucrose by 39±7% and to fluorescein by 47±7% (Pe values: sucrose control 7.373±0.617 ×10^{-3} cm/min, treated 4.496±0.530; fluorescein control 5.210±0.472, treated 2.781±0.395 ×10^{-3} cm/min). Permeability to FITC-dextrans of 4, 10, 20, 40, 70, 150 kDa was also reduced, with significant reduction for FD20 (20 kDa) from 0.333±0.031 to 0.156±0.013 ×10^{-3} cm/min. [1] Pore analysis indicated a decrease in number of large pores (~185 Å radius) and reduction of small pore radius from ~14.5 Å to ~8.3 Å following treatment. [1] Western blot analysis showed increased expression of tight junction proteins ZO-1 (225 kDa) and occludin (65 kDa) in treated cells. No change in expression of α-, β-, γ-catenin or p100/p120. [1] Immunofluorescence revealed improved continuity of ZO-1 at cell-cell contacts; occludin remained low but became detectable at junctions after treatment. [1] TRITC-phalloidin staining showed redistribution of F-actin from cytoplasmic stress fibers to cell periphery; cortactin similarly relocalized to cell-cell contacts. [1] No change in expression of actin-binding proteins cortactin, ezrin, or tyrosine kinase c-Src was observed by Western blot. [1] Dexamethasone Sodium Phosphate treatment did not alter transendothelial electrical resistance (remained ~66±3 Ω cm²). [1] |
| ln Vivo |
Dexamethasone (2 mg/kg) reduces the number of the BrdU-labeled hepatocytes by 80% in male Fischer F344 rats. Dexamethasone (2 mg/kg) pretreatment suppresses the expression of both TNF and IL-6 after partial hepatectomy and significantly reduces the proliferative response of the hepatocytes in male Fischer F344 rats. Dexamethasone also severely diminishes the induction and expansion of oval cells induced by the 2-acetylaminofluorene/partial hepatectomy (AAF/PH) protocol but does not have any effect on the proliferation of the bile duct cells stimulated by bile duct ligation. Dexamethasone (100 μg/kg) produces a significant decrease 59.2% of BrdU(+) hippocampal progenitor cells in Sprague–Dawley rats. Dexamethasone (100 μg/kg) decreases ERK activation in granule cell layer in Sprague–Dawley rats.
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| Cell Assay |
Dexamethasone Sodium Phosphate (as dexamethasone) was used in cell-based assays only. GPNT cells (immortalized rat brain endothelial line) were grown to confluence on collagen-coated Transwell-Clear inserts (polyester, 12 mm diameter, 0.4 μm pore size) or six-well plates in DMEM:Ham's F12 (1:1) medium containing 10% fetal calf serum, 10 mM HEPES, 100 U/mL penicillin, 100 μg/mL streptomycin, with or without 1 μM Dexamethasone Sodium Phosphate added from seeding. [1]
Paracellular permeability measurement: Monolayers on Transwell inserts were incubated with tracer markers ([14C]sucrose, fluorescein, FITC-dextrans of 4,10,20,40,70,150 kDa) in the apical compartment. Samples were taken from basolateral compartment at timed intervals. Permeability coefficients (Pe) were calculated from the slope of cleared volume vs. time curves. Values were corrected for unconjugated fluorescein in dextran preparations. [1] Transendothelial electrical resistance (TEER) measurement: Confluent GPNT monolayers on Transwell inserts were measured using an Endohm 12 chamber and Endohmeter; resistance was 66±3 Ω cm², unchanged by dexamethasone. [1] Immunofluorescence: Cells were fixed and stained with antibodies against ZO-1, occludin, β-catenin, p100/p120, and TRITC-phalloidin for F-actin, and anti-cortactin. Images were acquired. [1] Western blot: Whole cell lysates were prepared by replacing culture medium with hot SDS sample buffer, heated at 95°C for 5 min. Extracts were resolved by SDS-PAGE, transferred to nitrocellulose, blocked with 5% non-fat milk, probed with primary antibodies (anti-ZO-1, anti-occludin, anti-α/β/γ-catenin, anti-p100/p120, anti-cortactin, anti-ezrin, anti-c-Src), then HRP-conjugated secondary antibodies, and detected by enhanced chemiluminescence. [1] |
| Animal Protocol |
Dissolved in saline; 100 μg/kg; i.p. injection Sprague-Dawley rats
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| References |
Neurosci Lett.2003 Jun 26;344(2):112-6;J Physiol.2003 Feb 15;547(Pt 1):61-6.
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| Additional Infomation |
Dexamethasone sodium phosphate is an organosodium salt, the disodium salt of dexamethasone phosphate. It is a glucocorticoid receptor agonist. It contains the dexamethasone (2-) ion. Dexamethasone sodium phosphate is the sodium phosphate form of dexamethasone, a synthetic adrenocortical hormone with potent anti-inflammatory properties. In addition to binding to specific nuclear steroid receptors, dexamethasone can interfere with NF-κB activation and apoptosis pathways. Compared to other related adrenal hormones, this drug does not have sodium-retaining effects. (NCI04) See also: Dexamethasone (broadly defined); Dexamethasone sodium phosphate; Neomycin sulfate (ingredient)... See more...
Dexamethasone Sodium Phosphate (as dexamethasone) is a synthetic corticosteroid that modulates tight junction permeability in brain endothelial cells via glucocorticoid receptor-mediated transcriptional regulation. It may upregulate ZO-1 and occludin gene expression or downregulate mediators that increase permeability (e.g., MMP-9, VEGF). The effect is cell-type specific; similar observations have been reported in retinal endothelial cells with hydrocortisone, but not in mammary epithelial cells where actin/ZO-1 distribution was unchanged. [1] |
| Molecular Formula |
C22H30FO8P.2NA
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| Molecular Weight |
516.4
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| Exact Mass |
516.13
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| CAS # |
55203-24-2
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| Related CAS # |
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| PubChem CID |
16961
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
2.889
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
34
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| Complexity |
962
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| Defined Atom Stereocenter Count |
8
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| SMILES |
O=C1C=C2CC[C@H]3[C@@H]4C[C@@H](C)[C@@](C(COP([O-])([O-])=O)=O)(O)[C@@]4(C)C[C@H](O)[C@]3(F)[C@@]2(C)C=C1.[Na+].[Na+]
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| InChi Key |
PLCQGRYPOISRTQ-FCJDYXGNSA-L
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| InChi Code |
InChI=1S/C22H30FO8P.2Na/c1-12-8-16-15-5-4-13-9-14(24)6-7-19(13,2)21(15,23)17(25)10-20(16,3)22(12,27)18(26)11-31-32(28,29)30;;/h6-7,9,12,15-17,25,27H,4-5,8,10-11H2,1-3H3,(H2,28,29,30);;/q;2*+1/p-2/t12-,15+,16+,17+,19+,20+,21+,22+;;/m1../s1
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| Chemical Name |
disodium;[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] phosphate
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9365 mL | 9.6824 mL | 19.3648 mL | |
| 5 mM | 0.3873 mL | 1.9365 mL | 3.8730 mL | |
| 10 mM | 0.1936 mL | 0.9682 mL | 1.9365 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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