产品
编 号：F762967
分子式：C23H22Cl2N4O
分子量：441.35
分子式：C23H22Cl2N4O
分子量：441.35
产品类型
规格
价格
是否有货
1mg
询价
询价
5mg
询价
询价
10mg
询价
询价
25mg
询价
询价
结构图
CAS No: 3031837-35-8
产品详情
生物活性：
JAK-IN-23 is an orally active double inhibitor of JAK/STAT and NF-κB. JAK-IN-23 can inhibit JAK1/2/3 with IC50 values of 8.9 nM, 15 nM and 46.2 nM, respectively. JAK-IN-23 has potent inhibitory activities against interferon-stimulated genes (ISG) and NF-κB pathways with IC50 values of 3.3 nM and 150.7 nM, respectively. JAK-IN-23 has great anti-inflammatory that decreases the release of various proinflammatory factors. JAK-IN-23 can be used for the research of inflammatory bowel disease (IBD).
体内研究：
JAK-IN-23 (1-5 mg/kg, oral) produces a strong anti-inflammatory activity in both dextran sulfate sodium (DSS) - and 2,4,6-trinitrobenzenesulfonic acid (TNBS)-induced acute enteritis models and restores the structural composition of gut microbiota.Animal Model:DSS-Induced Acute Colitis Mice Model
Dosage:1 mg/kg, 3 mg/kg
Administration:oral
Result:Significantly decreased the DAI scores (1 and 3 mg/kg).Recovered the length of the colon (3 mg/kg).Significantly reduced the histopathology of ulcerative colitis (1 and 3 mg/kg).
Animal Model:The BALB/c mouse inflammatory bowel disease (IBD)model
Dosage:1 mg/kg, 5 mg/kg
Administration:oral
Result:Significantly improved the survival probability, had low DAI scores and effectively relieved symptoms of colitis in the TNBS-induced IBD mice model (5 mg/kg).Did not improve the survival probability and decreases the DAI score (100 mg/kg).
体外研究：
JAK-IN-23 inhibits JAK1/2/3 with IC50 values of 8.9 nM, 15 nM and 46.2 nM, respectively.JAK-IN-23 shows potent inhibitory activities against ISG and NF-KB with IC50 values of 3.3 nM and 150.7 nM, respectively.WB--- JAK-IN-23 (0.33μM, 1μM, 3μM; 24 h) can simultaneously block JAK-STAT1/3 and NF-κB proinflammatory signaling pathways in THP1-dual cells.JAK-IN-23 (0.003-3 μM; 24 h) decreases the release of various proinflammatory factors, including IL-6, IL-8, IL-1β in THP1-dual cells stimulated by LPS.JAK-IN-23 (0.11-3 μM; 24 h) decreases the release of various proinflammatory factors, including TNF-α, IL-12, IL-10 and IFNγ in LPS-induced peripheral blood mononuclear cells (PBMCs).JAK-IN-23 (1 μM) inhibits the expression of a variety of inflammation-related genes induced by LPS, including IL-1B, TNF, IL12B, and IL-23A and has inhibitory effects on the expression of genes involved in the unfolded protein response that was induced by LPS (1 μg/mL).
JAK-IN-23 is an orally active double inhibitor of JAK/STAT and NF-κB. JAK-IN-23 can inhibit JAK1/2/3 with IC50 values of 8.9 nM, 15 nM and 46.2 nM, respectively. JAK-IN-23 has potent inhibitory activities against interferon-stimulated genes (ISG) and NF-κB pathways with IC50 values of 3.3 nM and 150.7 nM, respectively. JAK-IN-23 has great anti-inflammatory that decreases the release of various proinflammatory factors. JAK-IN-23 can be used for the research of inflammatory bowel disease (IBD).
体内研究：
JAK-IN-23 (1-5 mg/kg, oral) produces a strong anti-inflammatory activity in both dextran sulfate sodium (DSS) - and 2,4,6-trinitrobenzenesulfonic acid (TNBS)-induced acute enteritis models and restores the structural composition of gut microbiota.Animal Model:DSS-Induced Acute Colitis Mice Model
Dosage:1 mg/kg, 3 mg/kg
Administration:oral
Result:Significantly decreased the DAI scores (1 and 3 mg/kg).Recovered the length of the colon (3 mg/kg).Significantly reduced the histopathology of ulcerative colitis (1 and 3 mg/kg).
Animal Model:The BALB/c mouse inflammatory bowel disease (IBD)model
Dosage:1 mg/kg, 5 mg/kg
Administration:oral
Result:Significantly improved the survival probability, had low DAI scores and effectively relieved symptoms of colitis in the TNBS-induced IBD mice model (5 mg/kg).Did not improve the survival probability and decreases the DAI score (100 mg/kg).
体外研究：
JAK-IN-23 inhibits JAK1/2/3 with IC50 values of 8.9 nM, 15 nM and 46.2 nM, respectively.JAK-IN-23 shows potent inhibitory activities against ISG and NF-KB with IC50 values of 3.3 nM and 150.7 nM, respectively.WB--- JAK-IN-23 (0.33μM, 1μM, 3μM; 24 h) can simultaneously block JAK-STAT1/3 and NF-κB proinflammatory signaling pathways in THP1-dual cells.JAK-IN-23 (0.003-3 μM; 24 h) decreases the release of various proinflammatory factors, including IL-6, IL-8, IL-1β in THP1-dual cells stimulated by LPS.JAK-IN-23 (0.11-3 μM; 24 h) decreases the release of various proinflammatory factors, including TNF-α, IL-12, IL-10 and IFNγ in LPS-induced peripheral blood mononuclear cells (PBMCs).JAK-IN-23 (1 μM) inhibits the expression of a variety of inflammation-related genes induced by LPS, including IL-1B, TNF, IL12B, and IL-23A and has inhibitory effects on the expression of genes involved in the unfolded protein response that was induced by LPS (1 μg/mL).
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