Dexamethasone Phosphate disodium 是糖皮质激素受体激动剂。

Dexamethasone disodium phosphate is a water-soluble form of the synthetic glucocorticoid dexamethasone.

Dexamethasone regulates multiple transcription factors, including activator protein-1, nuclear factor-AT, and nuclear factor-kB, resulting in 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.

Treatment with Dexamethasone at a dose of 2×5 mg/kg efficiently inhibits lipopolysaccharide (LPS)-induced inflammation. In our experimental system, treatment with a single dose of Dexamethasone 10 mg/kg (i.p.) markedly decreases the recruitment of granulocytes and spontaneous production of oxygen radicals compared with animals expose to LPS and injected with solvent alone (saline). The effects are statistically significant when administered both 1 h before and 1 h after inhalation of LPS. The number of granulocytes in BALF decreased to levels comparable to healthy animals (given an aerosol of water)[3]. Rats treated with Dexamethasone consume less food and weighed less than control rats. Treated rats also weigh less than pair-fed animals though their food intake is similar. Five days of Dexamethasone injection result in a significant increase in both the liver mass (+42%) and the liver to body weight ratio (+65%). The wet weight of gastrocnemius muscle decreases 20% after 5 days of treatment, but it remains unaffected relative to body weight (g/100 g body weight), indicating that muscle weight loss paralleled body weight loss.

2392-39-4

C22H30FO8P

495.43

EGP437. Dex-Phos;EGP 437;地塞米松磷酸二钠;EGP-437

DMSO:1 mg/mL (1.94 mM),ultrasonic and warming and heat to 80°C
H2O:100 mg/mL (193.65 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years