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CAS No.: 2392-39-4

地塞米松磷酸钠 Catalog No. CSN16655

Synonyms: 地塞米松磷酸二钠;Dexamethasone 21-phosphate disodium salt;地塞米松磷酸钠

Dexamethasone sodium phosphate is an agonist of glucocorticoid receptor.

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生物活性

实验方案

技术信息

生物活性

描述Endothelial cells (EC) can regulate the permeability in brain endothelium which is helpful to overcome the restriction of drug delivery into the brain. Dexamethasone Sodium Phosphate is a phosphate form of Dexamethasone. Dexamethasone is a corticosteroid medication used in modulating tight junction permeability and interleukin receptor modulator with different EC50 values and IC50 values in different kind of cells. GPNT cells treated with 1 μM dexamethasone demonstrated no change in transendothelial resistance, which decreased the permeability and reduced the size of the small pore as well. Dexamethasone treatment can lead to IL-6 and RPM18226 repressions with IC50 values of 1.4 and 6.5 nM respectively. The binding Ki of glucocorticoid receptor (GR) and mineralocorticoid (MR) were 2.1 and 7.2 nM respectively. While in human SW1353 cells, dexamethasone treatment showed an IC50 of GR binding of 3.5nM, the IC50 for transrepression of IL-1 induced MMP-13 expression and transrepression HWB-TNFα were 1.8 and 21 nM respectively. In LPS stimulated human PBMCs, DM affected cytokine production with EC50 values ranging from 10 to 72 nM, while the values were ranged from 0.47 to 4.1 nM and from 0.92 to >200 nM in Anti-CD3 and PHA stimulated human PBMCs respectively. In human H13 cells, DM inhibited GR with EC50 of 9.7 nM, all together suggesting a good in vitro and in vivo anti-inflammatory activity of this compound . DM exposure in the 5-month-old ewes demonstrated unchanged blood pressure and eNOS RNA and protein levels, increased sensitivity to endothelin-1 (ET), enhanced acetylcholine-induced relaxation and abolished L-NAME suppressible vasodilatory response to ET, suggesting that DM led to endothelial dysfunction and vasodilatory compensation in these animals.
动物研究
剂量
Rat: 4 mg/kg^[3] (i.p.), 10 mg/kg^[4] (i.p.)

给药途径
i.p.
参考文献

动物研究
剂量	Rat: 4 mg/kg^[3] (i.p.), 10 mg/kg^[4] (i.p.)
给药途径	i.p.

[1] Vakalis N, Echiadis G, et al. Intravitreal combination of dexamethasone sodium phosphate and bevacizumab in the treatment of exudative AMD. Sci Rep. 2015 Feb 27;5:8627.
[2] Kintzel PE, Zhao T, et al. Stability of i.v. admixture containing metoclopramide, diphenhydramine hydrochloride, and dexamethasone sodium phosphate in 0.9% sodium chloride injection. Am J Health Syst Pharm. 2014 Dec 1;71(23):2061-5.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.9365 mL
- 9.6823 mL
- 19.3647 mL
- 5 mM
- 0.3873 mL
- 1.9365 mL
- 3.8729 mL
- 10 mM
- 0.1936 mL
- 0.9682 mL
- 1.9365 mL

技术信息

CAS号

2392-39-4

储存条件

粉末: Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C22H28FNa2O8P

运输

蓝冰

分子量

516.40

别名

地塞米松磷酸二钠;Dexamethasone 21-phosphate disodium salt;地塞米松磷酸钠

溶解度

DMSO	insoluble
Water	130.0 mg/mL (251.7 mM)

动物实验配方

0.5% CMC-Na

40 mg/mL

clear

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