Дексаметазона ацетат 1177-87-3

Молекулярный вес: 434,5 Дексаметазон - мощный синтетический член класса глюкокортикоидов стероидных препаратов и модулятор рецепторов интерлейкина, который обладает противовоспалительным и иммунодепрессивным действием. \ N Биологическая активность.

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.
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

Протокол (только для справки) Исследование на животных: [5]

Animal Models	Sprague-Dawley rats
Formulation	Saline
Dosages	100 μg/kg
Administration	Intraperitoneal injection

Конверсия различных модельных животных на основе BSA (значение на основе данных из проекта рекомендаций 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

Например, чтобы изменить дозу ресвератрола, используемую для мыши (22,4 мг / кг), на дозу, основанную на BSA для крысы, умножьте 22,4 мг / кг на коэффициент Km для мыши, а затем разделите на коэффициент Km для крыса. Этот расчет дает эквивалентную дозу ресвератрола для крыс 11,2 мг / кг.

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

Ссылки Blanco FJ, et al. J Rheumatol, 1999, 26 (6), 1366-1373. Ямамото К. и др. FEBS Lett, 2000, 465 (2-3), 103-106. [3] Рикард DJ и др. Дев Биол, 1994, 161 (1), 218-228. [4] Надь П. и др. Гепатология, 1998, 28 (2), 423-429. [5] Ким Дж. Б. и др. Brain Res, 2004, 1027 (1-2), 1-10. [6] Wu CY, et al. J Immunol. 1998, 161 (6), 2723-2730. Химическая информация

Molecular Weight (MW)	434.5
Formula	C24H31FO6
CAS No.	1177-87-3

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

Solubility (25°C) *	In vitro	DMSO	87 mg/mL (200.23 mM)
		Water	<1 mg/mL (
		Ethanol	20 mg/mL (46.02 mM)

Chemical Name	16α-Methyl-9α-fluoroprednisolone 21-acetate

Группа Продуктов : Другие > Ингибитор рецептора IL