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Immunology/Inflammation IL Receptor Dexamethasone

Dexamethasone

Catalog No. T1076   CAS 50-02-2
Synonyms: Dexamethasone (DHAP), Prednisolone F, Hexadecadrol, MK 125, NSC 34521

Dexamethasone is a glucocorticoid receptor agonist and an IL receptor modulator.Dexamethasone inhibits production of exosomes containing inflammatory microRNA-155 in lipopolysaccharide-induced macrophage inflammatory responses

Dexamethasone, CAS 50-02-2
Pack Size Availability Price/USD Quantity
10 mg In stock 15.00
25 mg In stock 20.00
50 mg In stock 28.00
100 mg In stock 35.00
200 mg In stock 42.00
500 mg In stock 50.00
1 g In stock 86.00
1 mL * 10 mM (in DMSO) In stock 54.00
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Purity 98.00%
Purity 99.90%
Purity 99.91%
Purity 99.77%
Biological Description
Chemical Properties
Storage & Solubility Information
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Description Dexamethasone is a glucocorticoid receptor agonist and an IL receptor modulator.Dexamethasone inhibits production of exosomes containing inflammatory microRNA-155 in lipopolysaccharide-induced macrophage inflammatory responses
Targets&IC50 Annexin A1 ,   Glucocorticoid Receptor ,   IL receptor ,   iNOS ,   MRP1 ,   NR
In vitro GM-CSF release from A549 cells was inhibited by dexamethasone (EC50 = 2.2 nM). The concentration-dependent ability of dexamethasone (EC50 = 36 nM) to induce transcription of the beta2-receptor was found to correlate with GR DNA binding and occurred at 10-100 fold higher concentrations than the inhibition of GM-CSF release [1]. Following treatment with 1 microM dexamethasone, there was a decrease in transmonolayer paracellular permeability mainly to sucrose, fluorescein, and dextrans of up to 20 KDa [2].
In vivo Kd values (mean+/-SE) for cortisol in human mononuclear leukocytes (HML) of hypertensive patients were higher than in control subjects (24.6 versus 17.5 nmol/L). Binding capacity (4978 versus 4131 sites/cell), Kd values for dexamethasone (6.7 versus 5.7 nmol/L), and IC50 values for dexamethasone (3.4 versus 3.1 nmol/L) and cortisol (12.2 versus 9.5 nmol/L) were not significantly different [3]. Powerful reduction of neutrophils in bronchoalveolar lavage fluid (BALF) was obtained by a single i.p. injection of dexamethasone (10 mg/kg), whereas treatment with N-acetylcysteine (NAC) only resulted in reduction of neutrophils when administered at a high dose (500 mg/kg). A significant decrease of tumour necrosis factor-alpha, IL-1alpha, IL-1beta IL-6, IL- 12p40, and MIP-1alpha mRNA when mice where treated with dexamethasone but not when treated with NAC [4].
Animal Research
NAC was administered at three different doses (10, 100 and 500 mg/kg body weight). At the highest concentration, the acidic pH of the NAC solution was adjusted by adding NaOH. Dexamethasone was administered as a single injection of 1 or 10 mg/kg. Both drugs were dissolved in saline and 400 μl were injected intraperitoneally, either 1 h before or 1 h after LPS exposure. In one experiment, NAC (100 and 500 mg/kg) was injected successively every 4·5 h, starting 1 h before challenge (five injections in total). A control group of LPS-exposed animals were injected intraperitoneally with solvent alone (saline). Intratracheal administration was performed by instillation of 100 μl NAC (50, 100 or 500 mg/kg) or dexamethasone (10 mg/kg) into the lungs of mice anaesthetized with 15 mg/kg Rapinovet (i.v.) [4].
Synonyms Dexamethasone (DHAP) , Prednisolone F , Hexadecadrol , MK 125 , NSC 34521
Purity 98.00%
Molecular Weight 392.46
Formula C22H29FO5
CAS No. 50-02-2

Storage

0-4℃ for short term (days to weeks), or -20℃ for long term (months).

Solubility Information

DMSO: 73 mg/mL (186 mM)

Ethanol: 6 mg/mL (15.28 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Solution 1

30% PEG400+0.5% Tween80+5% propylene glycol: 30 mg/mL

Citations

References and Literature
1. 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. 2. Romero IA, et al. Changes in cytoskeletal and tight junctional proteins correlate with decreased permeability induced by dexamethasone in cultured rat brain endothelial cells. Neurosci Lett. 2003 Jun 26;344(2):112-6. 3. Mulatero P, et al. Impaired cortisol binding to glucocorticoid receptors in hypertensive patients. Hypertension. 1997 Nov;30(5):1274-8. 4. 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. 5. Ding C, Fu S, Chen X, et al. Epigallocatechin gallate affects the proliferation of human alveolar osteoblasts and periodontal ligament cells, as well as promoting cell differentiation by regulating PI3K/Akt signaling pathway[J]. Odontology. 2021: 1-12. 6. Huang L, Li Q. Notoginsenoside R1 promotes differentiation of human alveolar osteoblasts in inflammatory microenvironment through inhibiting NF‑κB pathway and activating Wnt/β‑catenin pathway[J]. Molecular Medicine Reports. 2020, 22(6): 4754-4762. 7. Zhang, Depeng, et al. Tabersonine attenuates lipopolysaccharide-induced acute lung injury via suppressing TRAF6 ubiquitination[J]. Biochemical pharmacology. 2018 Aug;154:183-192. 8. Sun C, Li X, Guo E, et al. MCP-1/CCR-2 axis in adipocytes and cancer cell respectively facilitates ovarian cancer peritoneal metastasis[J]. Oncogene. 2019: 1-15. 9. Li M, Yu H. Identification of WP1066, an inhibitor of JAK2 and STAT3, as a Kv1. 3 potassium channel blocker[J]. . British Journal of Pharmacology. 2021

Related compound libraries

This product is contained In the following compound libraries:
Approved Drug Library Bioactive Compound Library Anti-cancer Compound Library Anti-infection Compound Library Autophagy Compound Library FDA-approved Drug Library Immunology/Inflammation Compound Library Cytokine Inhibitor Library GPCR Compound Library Anti-cancer Approved drug Library Anti-cancer Clinical Compound Library Fluorochemical Library Anti-Metabolism Disease Compound Library Preclinical Compound Library CNS-Penetrant Compound Library Nuclear-receptor Inhibitors Library Anti-cancer Active Compound library Anti-cancer Drug library Drug Repurposing Library NMPA-Approved Drug Library FDA Approved & Pharmacopeial Drug Library

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