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Dexamethasone (Synonyms: Hexadecadrol; Prednisolone F)

目录号: HY-14648 纯度: 99。86%
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Dexamethasone 是一种糖皮质激素受体 (glucocorticoid receptor) 激动剂。

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Dexamethasone Chemical Structure

Dexamethasone Chemical Structure

CAS No. : 50-02-2

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Description

Dexamethasone is a glucocorticoid receptor agonist.

IC50 & Target

Glucocorticoid receptor[1]

In Vitro

Dexamethasone 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

It has previously been reported that 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.) significantly decreases recruitment of granulocytes as well as 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[4].

Clinical Trial
Storage

4°C, protect from light

Solvent & Solubility
In Vitro: 

DMSO : ≥ 56 mg/mL (142.69 mM)

H2O : < 0.1 mg/mL (insoluble)

* "≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 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
* 请根据产品在不同溶剂中的溶解度,选择合适的溶剂配制储备液,并请注意储备液的保存方式和期限。
In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案,配制前请先配制澄清的储备液,再依次添加助溶剂 (为保证实验结果的可靠性,体内实验的工作
液,建议您现用现配,当天使用;澄清的储备液可以根据储存条件,适当保存;以下溶剂前的百分比是指该溶剂在您配制终溶液中的体积占比):

  • 1.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.37 mM); Clear solution

  • 2.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (6.37 mM); Clear solution

  • 3.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2。5 mg/mL (6。37 mM); Clear solution

*以上所有助溶剂都可在 MCE 网站选购。
References
  • [1].

    [2].

    [3].

    [4]。

    [5]。

Animal Administration
[3][4]

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 anaesthetized with 15 mg/kg Rapinovet (i.v.).
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.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
  • [1].

    [2]。

    [3].

    [4]。

    [5]。

Molecular Weight

392.46

Formula

C₂₂H₂₉FO₅

CAS No.

50-02-2

SMILES

O=C1C=C[C@@]2(C)C(CC[C@]3([H])[C@]2(F)[C@@H](O)C[C@@]4(C)[C@@]3([H])C[C@@H](C)[C@@]4(C(CO)=O)O)=C1

Shipping

Room temperature in continental US; may vary elsewhere

Purity: 99.86%

  • [1].

    [2].

    [3].

    [4].

    [5].

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产品名称:
Dexamethasone
目录号:
HY-14648
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Dexamethasone

Cat. No.: HY-14648

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