Description du produit Poids moléculaire : 516,4 La dexaméthasone est un puissant membre synthétique de la classe des glucocorticoïdes des stéroïdes et un modulateur des récepteurs de l'interleukine qui a des effets anti-inflammatoires et immunosuppresseurs.
Activité biologique

Description	Dexamethasone is a potent synthetic member of the glucocorticoid class of steroid drugs, and an interleukin receptor modulator that has anti-inflammatory and immunosuppressant effects.
Targets	IL receptor [6]	COX-2 [1]
In vitro	Dexamethasone inhibits COX-2 mRNA expression induced by IL-1 in human articular chondrocytes. [1] Dexamethasone suppresses the cyclooxygenase-2 induction by tumor necrosis factor α (TNFα) with an IC50 of 1 nM in MC3T3-E1 cells. Dexamethasone binds to the glucocorticoid receptor and then to the glucocorticoid response element. [2]Dexamethasone (10 μM) induces osteoblastic differentiation of rat bone marrow stromal cell cultures with elevated mRNA expression of alkaline phosphatase osteopontin, bone sialoprotein, and osteocalcin. [3] Dexamethasone (5 μM) treatment decreases proliferation of adult hippocampal neural progenitor cells and SRE-driven gene expression. [5]
In vivo	Dexamethasone (2 mg/kg) reduces the number of the BrdU-labeled hepatocytes by 80% in male Fischer F344 rats. Dexamethasone (2 mg/kg) pretreatment suppresses the expression of both TNF and IL-6 after partial hepatectomy and significantly reduces the proliferative response of the hepatocytes in male Fischer F344 rats. Dexamethasone also severely diminishes the induction and expansion of oval cells induced by the 2-acetylaminofluorene/partial hepatectomy (AAF/PH) protocol but does not have any effect on the proliferation of the bile duct cells stimulated by bile duct ligation. [4] Dexamethasone (100 μg/kg) produces a significant decrease 59.2% of BrdU(+) hippocampal progenitor cells in Sprague–Dawley rats. Dexamethasone (100 μg/kg) decreases ERK activation in granule cell layer in Sprague–Dawley rats. [5]
Features	Great selectivity for COX-2.

Protocole (uniquement pour référence) Étude animale : [5]

Animal Models	Sprague-Dawley rats
Formulation	Saline
Dosages	100 μg/kg
Administration	Intraperitoneal injection
Solubility	Saline, 30 mg/mL
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Conversion de différents animaux modèles sur la base de la BSA (valeur basée sur les données des lignes directrices provisoires de la FDA)

Species	Baboon	Dog	Monkey	Rabbit	Guinea pig	Rat	Hamster	Mouse
Weight (kg)	12	10	3	1.8	0.4	0.15	0.08	0.02
Body Surface Area (m2)	0.6	0.5	0.24	0.15	0.05	0.025	0.02	0.007
Km factor	20	20	12	12	8	6	5	3

Animal A (mg/kg) = Animal B (mg/kg) multiplied by	Animal B Km
	Animal A Km

Par exemple, pour modifier la dose de resvératrol utilisée pour une souris (22,4 mg/kg) à une dose basée sur la BSA pour un rat, multiplier 22,4 mg/kg par le facteur Km pour une souris puis diviser par le facteur Km pour un rat. Ce calcul donne une dose équivalente chez le rat pour le resvératrol de 11,2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×	mouse Km(3)	= 11.2 mg/kg
	rat Km(6)

1 Références [1] Blanco FJ, et al. J Rheumatol, 1999, 26(6), 1366-1373. [2] Yamamoto K, et al. FEBS Lett, 2000, 465(2-3), 103-106. [3] Rickard DJ, et al. Dev Biol, 1994, 161(1), 218-228. [4] Nagy P, et al. Hépatologie, 1998, 28(2), 423-429. [5] Kim JB, et al. Brain Res, 2004, 1027(1-2), 1-10. [6] Wu CY, et al. J Immunol. 1998, 161(6), 2723-2730.
Informations chimiques

Molecular Weight (MW)	516.4
Formula	C22H30FO8P.2Na
CAS No.	55203-24-2

Storage	3 years -20℃Powder
	6 months-80℃in solvent (DMSO, water, etc.)
Synonyms

Solubility (25°C) *	In vitro	DMSO	<1 mg/mL (
		Water	103 mg/mL (199.45 mM)
		Ethanol	<1 mg/mL (
	In vivo	Saline	30 mg/mL

Chemical Name	Pregna-1,4-diene-3,20-dione, 9-fluoro-11,17-dihydroxy-16-methyl-21-(phosphonooxy)-, sodium salt (1:2), (11β,16α)-

Groupes de Produits : Autres > Inhibiteur du récepteur IL