1. Materials information
Names
| Name |
Dexamethasone-17-acetate
|
| Synonym |
More Synonyms
|
Dexamethasone-17-acetate Biological Activity
| Description |
Dexamethasone acetate is a glucocorticoid receptor agonist. |
| Related Catalog |
Signaling Pathways >>
Autophagy >>
Autophagy
Signaling Pathways >>
GPCR/G Protein >>
Glucocorticoid Receptor
Signaling Pathways >>
Autophagy >>
Mitophagy
Research Areas >>
Inflammation/Immunology
|
| 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].
|
| Animal Admin |
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.
|
| 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. [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 [3]. 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 [4]. Roussel
D, et al. Dexamethasone treatment specifically increases the basal
proton conductance of rat liver mitochondria. FEBS Lett. 2003 Apr
24;541(1-3):75-9.
|
Chemical & Physical Properties
| Density |
1.3±0.1 g/cm3 |
| Boiling Point |
579.4±50.0 °C at 760 mmHg |
| Melting Point |
238-240 °C(lit.) |
| Molecular Formula |
C24H31FO6 |
| Molecular Weight |
434.498 |
| Flash Point |
304.2±30.1 °C |
| Exact Mass |
434.210480 |
| PSA |
100.90000 |
| LogP |
2.96 |
| Vapour Pressure |
0.0±3.6 mmHg at 25°C |
| Index of Refraction |
1.571 |
| Storage condition |
2-8°C |
2. Packaging of materials
For powders: normal is 25kgs/Drum or bag, or larger/smaller package as request.
For liquids: normal 25kgs/drum, 180-300kgs/bucket, or IBC, determined by the nature of the product.
Or smaller package 1kg/bottle, 10kgs/bottle as request.
3. Shipping & Delivery
Provide door to door service
Suitable for goods under 50kg
Delivery: 3-7 days
Cost: low cost
Provide airport to airport service
Suitable for goods over 50kg
Delivery: 3-14 days
Cost: high cost
Provide seaport to seaport service
Suitable for goods over 100kg
Delivery: 2-45 days
Cost: low cost
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