Peso molecular: 434,5 La dexametasona es un potente miembro sintético de la clase de glucocorticoides de fármacos esteroides y un modulador del receptor de interleucina que tiene efectos antiinflamatorios e inmunosupresores. \ N Actividad biológica
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Description
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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.
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In vitro
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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]
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In vivo
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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]
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Features
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Protocolo (solo como referencia) Estudio en animales: [5]
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Animal Models
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Sprague-Dawley rats
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Formulation
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Saline
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Dosages
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100 μg/kg
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Administration
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Intraperitoneal injection
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Conversión de diferentes modelos de animales basados en BSA (valor basado en datos del Borrador de Directrices de la FDA)
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Species
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Baboon
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Dog
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Monkey
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Rabbit
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Guinea pig
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Rat
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Hamster
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Mouse
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Weight (kg)
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12
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10
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3
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1.8
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0.4
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0.15
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0.08
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0.02
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Body Surface Area (m2)
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0.6
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0.5
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0.24
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0.15
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0.05
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0.025
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0.02
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0.007
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Km factor
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20
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20
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12
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12
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8
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6
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5
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3
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Animal A (mg/kg) = Animal B (mg/kg) multiplied by
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Animal B Km
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Animal A Km
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Por ejemplo, para modificar la dosis de resveratrol utilizada para un ratón (22,4 mg / kg) a una dosis basada en el BSA para una rata, multiplique 22,4 mg / kg por el factor Km para un ratón y luego divida por el factor Km para una rata. Este cálculo da como resultado una dosis equivalente para ratas de resveratrol de 11,2 mg / kg.
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Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×
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mouse Km(3)
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= 11.2 mg/kg
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rat Km(6)
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Referencias Blanco FJ, et al. J Rheumatol, 1999, 26 (6), 1366-1373. Yamamoto K, et al. FEBS Lett, 2000, 465 (2-3), 103-106. [3] Rickard DJ y col. Dev Biol, 1994, 161 (1), 218-228. [4] Nagy P y col. Hepatología, 1998, 28 (2), 423-429. [5] Kim JB y col. Brain Res, 2004, 1027 (1-2), 1-10. [6] Wu CY y col. J Immunol. 1998, 161 (6), 2723-2730. Información química
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Molecular Weight (MW)
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434.5
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Formula
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C24H31FO6
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CAS No.
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1177-87-3
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Storage
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3 years -20℃Powder
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6 months-80℃in solvent (DMSO, water, etc.)
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Synonyms
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Solubility (25°C) *
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In vitro
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DMSO
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87 mg/mL
(200.23 mM)
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Water
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<1 mg/mL
(
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Ethanol
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20 mg/mL
(46.02 mM)
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Chemical Name
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16α-Methyl-9α-fluoroprednisolone 21-acetate
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Grupos de Producto : Otros > Inhibidor del receptor de IL
