| Size | Price | Stock | Qty |
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| 500mg |
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Purity: ≥98%
Dexamethasone (also known as DHAP; Hexadecadrol; Prednisolone F)) is a potent synthetic glucocorticoid class of steroid drugs, and an interleukin receptor modulator with anti-inflammatory and immunosuppressive activities. Dexamethasone has anti-inflammatory and immunosuppressant effects. It is 25-fold more potent than cortisol in its glucocorticoid effect, while having minimal mineralocorticoid effect. Dexamethasone is used for the treatment of many conditions including: rheumatologic problems, a number of skin diseases such as erythema multiforme, severe allergies, asthma etc.
| ln Vitro |
Dexamethasone, also known as hexadecadrol, acts as a regulator of several transcription factors, including as nuclear factor-AT, nuclear factor-kB, and activator protein-1, which in turn activates and inhibits important genes related to the inflammatory response [1]. With an EC50 of 2.2 nM, dexamethasone efficiently prevents A549 cells from releasing granulocyte-macrophage colony-stimulating factor (GM-CSF). At dosages greater than those that suppress GM-CSF production, dexamethasone (EC50=36 nM) is shown to be related with glucocorticoid receptor (GR) DNA binding, happening 10-100-fold higher. It also promotes β2 receptor transcription. The inhibition of GM-CSF release is linked to the inhibition of 3×κB (NF-κB, IκBα, and I-κBβ) by dexamethasone (IC50=0.5 nM) [2].
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| ln Vivo |
Dexamethasone can be used to create models of nerve injury, muscular atrophy, and mitochondrial diseases in animals. It has been previously documented that lipopolysaccharide (LPS)-induced inflammation can be effectively inhibited by treatment with dexamethasone (Hexadecadrol) at a dose of 2 × 5 mg/kg. When compared to mice exposed to lipopolysaccharide (LPS) and injected with vehicle (saline) alone, treatment with a single dosage of dexamethasone 10 mg/kg (ip) dramatically decreased the recruitment of granulocytes and the spontaneous generation of oxygen radicals in our experimental system. The impact was statistically significant when given one hour prior to and one hour following LPS inhalation. By administering water aerosol, the quantity of granulocytes in BALF is lowered to levels similar to those in healthy animals [3]. Dexamethasone-treated rats ate less food and weighed less than rats in the control group. Despite eating the same amount of food, the treated rats weighed less than the animals fed in pairs. Dexamethasone injections for five days caused a notable rise in liver mass (+42%) and the liver-to-body weight ratio (+65%). After five days of treatment, the wet weight of the gastrocnemius muscle dropped by 20%, but it did not change in relation to body weight (g/100 g body weight), suggesting that weight reduction and muscle weight loss were synchronized [4].
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| References |
[1]. LaLone CA, et al. Effects of a glucocorticoid receptor agonist, Dexamethasone, on fathead minnow reproduction, growth, and development. Environ Toxicol Chem. 2012 Mar;31(3):611-22.
[2]. Adcock IM, et al. Ligand-induced differentiation of glucocorticoid receptor (GR) trans-repression and transactivation: preferential targetting of NF-kappaB and lack of I-kappaB involvement. Br J Pharmacol. 1999 Jun;127(4):1003-11 [3]. Rocksén D, et al. Differential anti-inflammatory and anti-oxidative effects of Dexamethasone and N-acetylcysteine in endotoxin-induced lung inflammation. Clin Exp Immunol. 2000 Nov;122(2):249-56 [4]. Roussel D, et al. Dexamethasone treatment specifically increases the basal proton conductance of rat liver mitochondria. FEBS Lett. 2003 Apr 24;541(1-3):75-9. [5]. Ballabh P, et al. Neutrophil and monocyte adhesion molecules in bronchopulmonary dysplasia, and effects of corticosteroids. Arch Dis Child Fetal Neonatal Ed. 2004 Jan;89(1):F76-83. [6]. Heidi Ledford. et al. Coronavirus Breakthrough: Dexamethasone Is First Drug Shown to Save Lives. Nature. 2020 Jun 16. [7]. Yun Chen, et al. Glucocorticoids inhibit production of exosomes containing inflammatory microRNA-155 in lipopolysaccharide-induced macrophage inflammatory responses. Int J Clin Exp Pathol 2018;11(7):3391-3397 |
| Molecular Formula |
C22H29FO5
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| Molecular Weight |
392.46
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| CAS # |
50-02-2
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| Related CAS # |
3936-02-5 (metasulfobenzoate sodium);3800-84-8 (sodium succinate);1177-87-3 (acetate);150587-07-8 (beloxil); 132245-57-9 (cipecilate); 2265-64-7 (isonicotinate); 14899-36-6 (palmitate); 312-93-6 (phosphate); 2392-39-4 (sodium phosphate);
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| SMILES |
F[C@@]12[C@]3(C([H])=C([H])C(C([H])=C3C([H])([H])C([H])([H])[C@@]1([H])[C@]1([H])C([H])([H])[C@@]([H])(C([H])([H])[H])[C@](C(C([H])([H])O[H])=O)([C@@]1(C([H])([H])[H])C([H])([H])[C@]2([H])O[H])O[H])=O)C([H])([H])[H]
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
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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) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.37 mM) (saturation unknown) in 5% DMSO + 95% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
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. Solubility in Formulation 2: ≥ 2.08 mg/mL (5.30 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. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (5.30 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: ≥ 2.08 mg/mL (5.30 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. 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 corn oil and mix evenly. Solubility in Formulation 5: 30% PEG400+0.5% Tween80+5% Propylene glycol : 30mg/kg Solubility in Formulation 6: 18.18 mg/mL (46.32 mM) in 0.5% CMC-Na/saline water (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5480 mL | 12.7402 mL | 25.4803 mL | |
| 5 mM | 0.5096 mL | 2.5480 mL | 5.0961 mL | |
| 10 mM | 0.2548 mL | 1.2740 mL | 2.5480 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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