产品
编 号：F019466
分子式：C24H29N3O4
分子量：423.5
分子式：C24H29N3O4
分子量：423.5
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规格
价格
是否有货
10mM*1mL in DMSO
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1mg
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5mg
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10mg
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25mg
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50mg
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100mg
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结构图
CAS No: 1044871-04-6
产品详情
生物活性：
RVX-297 is a potent, orally active BET bromodomain inhibitor with selectivity for BD2. RVX-297 shows IC50s of 0.08, 0.05, and 0.02 μM for BRD2(BD2), BRD3(BD2), and BRD4(BD2), respectively. RVX-297 suppresses inflammatory gene expression in multiple immune cell types. RVX-297 is effective in acute inflammation and autoimmunity models.
体内研究：
RVX-297 (25-75 mg/kg; p.o.; per day for 6 day) inhibits progression of pathology in the rat collagen-induced arthritis model.RVX-297 (75-150 mg/kg) inhibits progression of pathology in the mouse collagen-induced arthritis model.RVX-297 suppresses cytokine production in LPS-treated mice.Animal Model:Female Lewis rats are 6-8 weeks old, approximately 150 g (rat collagen-induced arthritis)
Dosage:25, 50, and 75 mg/kg
Administration:P.o.; per day for 6 days
Result:Prevented swelling and inflammation of the ankle and knee joints.
体外研究：
RVX-297 (1-30 μM; 24 hours) decreases proinflammatory gene expression in synovial fibroblasts.RVX-297 displaces BET proteins from the promoters of sensitive genes and disrupted recruitment of active RNA polymerase II, a property shared with pan-BET inhibitors that nonselectively bind BET BDs. RVX-297 reduces gene expression of inflammatory mediators in vitro. RVX-297 suppresses IL-6 gene induction in human U937 macrophages, mouse primary B cells isolated from the spleen, mouse BMDMs, and THP-1 monocytes in a dose-dependent manner. RVX-297 represses IL-1β expression in LPS-stimulated mouse BMDMs, with an IC50 of 0.4-3 μM. RVX-297 inhibits MCP-1 expression in unstimulated human PBMCs with an IC50 of 0.4 μM. RVX-297 inhibits antigen stimulation of T cells and the induction of IL-17 expression.
RVX-297 is a potent, orally active BET bromodomain inhibitor with selectivity for BD2. RVX-297 shows IC50s of 0.08, 0.05, and 0.02 μM for BRD2(BD2), BRD3(BD2), and BRD4(BD2), respectively. RVX-297 suppresses inflammatory gene expression in multiple immune cell types. RVX-297 is effective in acute inflammation and autoimmunity models.
体内研究：
RVX-297 (25-75 mg/kg; p.o.; per day for 6 day) inhibits progression of pathology in the rat collagen-induced arthritis model.RVX-297 (75-150 mg/kg) inhibits progression of pathology in the mouse collagen-induced arthritis model.RVX-297 suppresses cytokine production in LPS-treated mice.Animal Model:Female Lewis rats are 6-8 weeks old, approximately 150 g (rat collagen-induced arthritis)
Dosage:25, 50, and 75 mg/kg
Administration:P.o.; per day for 6 days
Result:Prevented swelling and inflammation of the ankle and knee joints.
体外研究：
RVX-297 (1-30 μM; 24 hours) decreases proinflammatory gene expression in synovial fibroblasts.RVX-297 displaces BET proteins from the promoters of sensitive genes and disrupted recruitment of active RNA polymerase II, a property shared with pan-BET inhibitors that nonselectively bind BET BDs. RVX-297 reduces gene expression of inflammatory mediators in vitro. RVX-297 suppresses IL-6 gene induction in human U937 macrophages, mouse primary B cells isolated from the spleen, mouse BMDMs, and THP-1 monocytes in a dose-dependent manner. RVX-297 represses IL-1β expression in LPS-stimulated mouse BMDMs, with an IC50 of 0.4-3 μM. RVX-297 inhibits MCP-1 expression in unstimulated human PBMCs with an IC50 of 0.4 μM. RVX-297 inhibits antigen stimulation of T cells and the induction of IL-17 expression.
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