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编 号:F340941
分子式:C17H21ClN4O3S2
分子量:428.96
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10mM*1mL in DMSO
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5mg
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10mg
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50mg
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100mg
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生物活性:
BVT 2733 is a potent, selective, and orally active non-steroidal 11β-hydroxydehydrogenase 1 (11β-HSD1) inhibitor. BVT 2733 is potently against the mouse enzyme (IC50=96 nM) over the human enzyme (IC50=3341 nM). BVT 2733 has the potential for the study of arthritis and obesity related disease.

体内研究:
BVT-2733 (oral administration; 100 mg/kg; twice daily; 2 weeks) attenuates the arthritis severity and anti-CII level and decreases the levels of serum TNF-α, IL-1β, IL-6 and IL-17 in CIA mice.BVT 2733 (oral administration; 100 mg/kg; dosed (09.00 and 17.00 h); last 4 weeks) exhibits decreased body weight and enhanced glucose tolerance and insulin sensitivity when it compares to control mice. It also down-regulated the expression of inflammation-related genes including monocyte chemoattractant protein 1 (MCP-1), tumor necrosis factor alpha (TNF-α) and the number of infiltrated macrophages within the adipose tissue in vivo.Animal Model:Collagen-induced arthritis (CIA)?mice
Dosage:100 mg/kg
Administration:Oral administration; twice daily; 2 weeks
Result:Reduced synovial inflammation and joint destruction.
Animal Model:C57BL/6J mice
Dosage:100 mg/kg
Administration:Oral administration; dosed (09.00 and 17.00 h); last 4 weeks
Result:Improved metabolic homeostasis and suppressed the inflammation of adipose tissue in diet-induced obese mice.?

体外研究:
BVT 2733 (100 μM; 24 hours) co-treatment with PA (100 μM) reduces MCP-1 expression in fully differentiation adipocytes.BVT 2733 (50-100 μM; 24 hours) reduces the inflammation protein levels (MCP-1, IL-6) in medium?in J774.1 macrophages by Elisa.
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