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Dexamethasone

MCE China：Dexamethasone

Brand：MedChemExpress (MCE)

Cat. No.HY-14648

CAS：50-02-2

Synonyms：Hexadecadrol; Prednisolone F

Purity：99.86%

Storage：4°C, protect from light *In solvent : -80°C, 1 year; -20°C, 6 months (protect from light)

Shipping：Room temperature in continental US; may vary elsewhere.

Description：Dexamethasone (Hexadecadrol) is a glucocorticoid receptor agonist, apoptosis inducer, and common disease inducer in experimental animals, constructing models of muscle atrophy, hypertension, and depression. Dexamethasone can inhibit the production of inflammatory miRNA-155 exosomes in macrophages and significantly reduce the expression of inflammatory factors in neutrophils and monocytes. Dexamethasone also has potential for use in COVID-19 research.

In Vitro：Dexamethasone (Hexadecadrol) regulates several transcription factors, including activator protein-1, nuclear factor-AT, and nuclear factor-kB, leading to the activation and repression of key genes involved in the inflammatory response[1]. Dexamethasone potently inhibits granulocyte-macrophage colony stimulating factor (GM-CSF) release from A549 cells with EC50 of 2.2 nM. Dexamethasone (EC50=36 nM) induces transcription of the β2-receptor is found to correlate with glucocorticoid receptor (GR) DNA binding and occurred at 10-100 fold higher concentrations than the inhibition of GM-CSF release. Dexamethasone (IC50=0.5 nM) inhibits a 3×κB (NF-κB, IκBα, and I-κBβ), which is associated with inhibition of GM-CSF release[2].

In Vivo：.f12{ font-size: 12px; } .fwb{ font-weight: bold; } .lh22{ line-height: 22px;; } .lh23 { line-height: 23px; } .pl13{ padding-left: 13px;; } .part { margin-top: 18px; } .mold-first-tit { width: 100%; height: 44px; line-height: 44px; background: #F9F7FB; border-bottom: 1px solid #EBE4F6; padding-left: 16px; box-sizing: border-box; margin-bottom: 17px; } .mold-second-tit:before { content:""; width: 6px; height: 6px; display: inline-block; border-radius: 50%; background: rgba(255,102,0,0.4); margin-right: 12px; position: relative; top: -3px; } .lft-border { border-left: 1px dotted #EBE4F6; padding-right: 12px; margin-left: 3px; box-sizing: border-box; padding-bottom: 12px; } /* .part .dec:last-child { border-bottom: 0; } */ .dec { margin: 10px 15px 0; padding-bottom: 10px; border-bottom: 1px dashed #EBE4F6; } .btm-border { border-left: 1px dashed #EBE4F6; } .text-bg { margin-top: 10px; background: #FFFBF1; padding: 14px; border-bottom: 0; position: relative; } .text-note-bg { margin-top: 10px; background: #FFFDF7; padding: 12px; border-bottom: 0; position: relative; } .text-note { width: 51px; height: 20px; line-height: 20px; background: #FFE2AA; text-align: center; border-radius: 0 0 8px 0; position: absolute; top: 0; left: 0; } .text-note-dec { margin-top: 15px;; } Based on blood and multi-tissue concentration-time profiles of Dexamethasone (DEX), no significant sex differences were found in its tissue distribution. Blood cell to plasma partitioning (0.664) and plasma free fraction (0.175) were moderate, with widespread distribution in the liver (Kp=6.76). Possibly due to P-glycoprotein-mediated efflux, the concentration of DEX in the brain is very low compared to the expected high permeability[5]. Dexamethasone (DEX) can be used in animal modeling to construct models of muscle atrophy, hypertension and depression. 1. Induction of muscle atrophy[6][7] Background Glucocorticoids are important mediators of skeletal muscle protein degradation and upregulation of the ubiquitin-proteasome pathway. Dexamethasone induces tibialis anterior muscle protein degradation by binding to the glucocorticoid receptor, resulting in muscle atrophy. Specific Mmodeling Methods Mice: C57BL/6 • male • 6-week-oldAdministration: 5 mg/kg • ip • once daily for 2 weeks Modeling Indicators Molecular changes: Increased indicators: C2C12 ubiquitin ligase, MuRF1, Atrogin-1, Cbl-b, p-Foxo1, p-Foxo3a. Resulted C2C12 myotube protein degradation, and Glucocorticoid receptor translocation to the nucleus Phenotypic observation: Decreased indicators: The weight of the anterior muscles, gastrocnemius, quadriceps and soleus muscles. The ratio of skeletal muscle to body weight decreases. Correlated Product(s): Betamethasone (HY-13570) Opposite Product(s): Glabridin (HY-N0393) 2. Induction of hypertension[8][9] Background The underlying mechanisms that induce hypertension (HT) are unknown. Specific Modeling Methods Rat: Sprague-Dawley • Male • 200-300 gAdministration: 20 μg • sc • once daily from days 5 to 16 • control rats: saline with 0.1 mL/100 g/day from days 1 to 16 (po) or 0.2 mL/rat/day (sc). Dog: 10.1-19.1 kg • average=13.7 kgAdministration: 0.5 mg/kg • po • once daily for 10 days Modeling Indicators b>Hemodynamics：MAP, systolic blood pressure, diastolic blood pressure, TPR levels increased in central hemodynamics. Total peripheral resistance, blood pressure, atrial natriuretic peptide, and the pressor response to norepinephrine, are significantly increased in Systemic and renal hemodynamics. Behavior: The dog showed obvious natriuresis and diuresis. Opposite Product(s): Saralasin (HY-P0205); Prazosin (HY-B0193) 3. Induction of depressive behavior[10][11] Background Astrocytes are a key feature of major depressive disorder (MD), and reduced expression by glucocorticoids results in reduced astrocyte numbers. Long-term treatment with Dexamethasone can cause a series of depression-like symptoms in rodents. Specific Modeling Methods Rat: Sprague-Dawley • Male • 200-250 gAdministration: 1 mg/kg • po • once daily every other day for 5 months Note (1) Prepare a 3% (w/v) treatment solution and filter through a 0.45 μm cellulose acetate filter. (2) Rats should not be exposed to any other water source for 4 days before starting treatment. (3) On the 4th day, change the treatment solution to water and feed for 3 days to allow the mice to recover temporarily. Weigh and conduct behavioral experiments on day 7. Mice: C57BL/6 • Male • 9-10 weeks old • 23-25 gAdministration: 4 mg/kg • ip • once dailly for 21 days Modeling Indicators Metabolism changes: Serum cortisol levels in rats ↑. Behavior: Immobility time during the forced swim test (FST) &uarr. Preference for sucrose &darr in the sucrose preference test. Opposite Product(s): Amitriptyline (HY-B0527)

Animal Administration：Mice[3] Female C57Bl/6JBom mice (age 10-12 weeks) are used in all experiments. Dexamethasone is administered as a single injection of 1 or 10 mg/kg. Dexamethasone is dissolved in saline and 400 μL are injected intraperitoneally, either 1 h before or 1 h after LPS exposure. In one experiment, N-acetylcysteine (NAC) (100 and 500 mg/kg) is injected successively every 4•5 h, starting 1 h before challenge (five injections in total). A control group of LPS-exposed animals are injected intraperitoneally with solvent alone (saline). Intratracheal administration is performed by instillation of 100 μL NAC (50, 100 or 500 mg/kg) or Dexamethasone (10 mg/kg) into the lungs of mice. Rats[4] Male Sprague-Dawley rats are used.Dexamethasone-treated rats are injected intraperitoneally once daily with Dexamethasone (1.5 mg/kg body weight) for 5 days and are allowed to feed ad libitum. The Dexamethasone dose (1.5 mg/kg/day) and the duration of treatment (5 days) are specifically chosen as this treatment induced a reproducible and marked catabolic state. Control rats received no treatment and are fed ad libitum. In order to take into account the decrease in food intake induced by Dexamethasone treatment, a third group of pair-fed rats are used. These rats are provided with the same amount of food as Dexamethasone-injected rats and are treated with a daily isovolumic intraperitoneal injection of NaCl (0.9%) for 5 days. After the final injection of Dexamethasone or NaCl, the animals are fasted overnight prior to being killed by decapitation.

IC50 & Target：Glucocorticoid receptor[1] Cellular Effect Cell Line Type Value Description References

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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.  [Content Brief]

[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  [Content Brief]

[3]. 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.  [Content Brief]

[4]. 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.

[5]. Song D, et al. Physiologically Based Pharmacokinetics of Dexamethasone in Rats. Drug Metab Dispos. 2020 Sep;48(9):811-818.  [Content Brief]

[6]. Yoshioka Y, et al. Glabridin inhibits dexamethasone-induced muscle atrophy. Arch Biochem Biophys. 2019 Mar 30;664:157-166.  [Content Brief]

[7]. Troncoso R, et al. Dexamethasone-induced autophagy mediates muscle atrophy through mitochondrial clearance. Cell Cycle. 2014;13(14):2281-95.  [Content Brief]

[8]. Ong SL, et al. Hemodynamics of dexamethasone-induced hypertension in the rat. Hypertens Res. 2009 Oct;32(10):889-94.  [Content Brief]

[9]. Nakamoto H, et al. Characterization of alterations of hemodynamics and neuroendocrine hormones in dexamethasone induced hypertension in dogs. Clin Exp Hypertens A. 1991;13(4):587-606.  [Content Brief]

[10]. Mesripour A, et al. The effect of vitamin B6 on dexamethasone-induced depression in mice model of despair. Nutr Neurosci. 2019 Oct;22(10):744-749.  [Content Brief]

[11]. Bhatt S, et al. Role of Aspirin and Dexamethasone against Experimentally Induced Depression in Rats. Basic Clin Pharmacol Toxicol. 2016 Jul;119(1):10-8.  [Content Brief]