Peso molecular: 434,5 A dexametasona é um potente membro sintético da classe dos glicocorticóides dos medicamentos esteróides e um modulador do receptor de interleucina que tem efeitos antiinflamatórios e imunossupressores. \ N Atividade 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 (apenas para referência) de estudo em animais: [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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Conversão de diferentes modelos de animais com base em BSA (valor com base em dados das diretrizes preliminares da 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 exemplo, para modificar a dose de resveratrol usada para um camundongo (22,4 mg / kg) para uma dose baseada na BSA para um rato, multiplique 22,4 mg / kg pelo fator Km para um camundongo e, em seguida, divida pelo fator Km para um rato. Este cálculo resulta em uma dose equivalente de rato para o 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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Referências 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, et al. Dev Biol, 1994, 161 (1), 218-228. [4] Nagy P, et al. Hepatology, 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. Informação 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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Grupo de Produto : Outros > Inibidor do receptor de IL
