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编 号：F754554
分子式：C30H30N4O2
分子量：478.58
分子式：C30H30N4O2
分子量：478.58
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CAS No: 2677039-24-4
产品详情
生物活性：
BET BD2-IN-1 (compound 45) is a potent and selective inhibitor of BET BD2 (IC50=1.6 nM). BET BD2-IN-1 inhibits the differentiation of Th17 cells by decreasing the activation of STAT3 and NF-κB. BET BD2-IN-1 is used in psoriasis and inflammatory bowel disease (IBD) research.
体内研究：
BET BD2-IN-1 (20 mg/kg，静脉注射；每日 1 次，连用 7 天) 可抑制小鼠皮肤组织中 p-STAT3 和 p-NF-κB 蛋白的表达，有效改善银屑病小鼠模型的病理改变。BET BD2-IN-1 (20 mg/kg，静脉注射；每日 1 次，连用 7 天) 显著降低 DSS 诱导的 IBD 小鼠模型疾病活动指数 (DAI) 评分。Pharmacokinetic Analysis of BET BD2-IN-1 in Sprague Dawley Rats ModelparameterAUC(0?t) (ng?h/mL)C0 (ng/mL)T1/2 (h)CL (mL/kg/min)Vdss (L/kg)
iv(1 mg/kg)272 ± 7.2279 ± 781.5 ± 0.160 ± 2.06.6 ± 0.8
parameterAUC(0?t) (ng?h/mL)Cmax (ng/mL)T1/2 (h)Tmax (h)F (%)
po(10 mg/kg)78 ± 3420 ± 111.9 ± 0.22.7 ± 1.2 2.9 ± 1.2
Animal Model:Imiquimod (HY-B0180)-induced Psoriasis mouse model
Dosage:10 and 20 mg/kg
Administration:Intravenous injection (i.v.) ; Once daily for seven days
Result:Significantly alleviated the Imiquimod-induced skin lesions in a dose-dependent manner. Obviously reduced the enlarged spleen. Significantly decreased the expression of p-STAT3 and p-NF-κB in mouse skin tissues.
Animal Model:DSS (HY-116282C)-induced IBD mouse model
Dosage:10 and 20 mg/kg
Administration:Intravenous injection (i.v.) ; Once daily for seven days
Result:Effectively prevented colon shortening. Effectively alleviated the DSS-induced weight loss. Significantly alleviated the infiltration of inflammatory cells, areas of ulceration as well as loss of mucosal epithelium, and goblet cells caused by DSS.
体外研究：
BET BD2-IN-1 (500 nM) 能有效抑制 Th17 细胞分化，对 BD2 的选择性优于 BD1。BET BD2-IN-1 (4 nM) 在完整细胞中与 BRD4 BD2 结合，对 BRD4 BD2 具有稳定效应。
BET BD2-IN-1 (compound 45) is a potent and selective inhibitor of BET BD2 (IC50=1.6 nM). BET BD2-IN-1 inhibits the differentiation of Th17 cells by decreasing the activation of STAT3 and NF-κB. BET BD2-IN-1 is used in psoriasis and inflammatory bowel disease (IBD) research.
体内研究：
BET BD2-IN-1 (20 mg/kg，静脉注射；每日 1 次，连用 7 天) 可抑制小鼠皮肤组织中 p-STAT3 和 p-NF-κB 蛋白的表达，有效改善银屑病小鼠模型的病理改变。BET BD2-IN-1 (20 mg/kg，静脉注射；每日 1 次，连用 7 天) 显著降低 DSS 诱导的 IBD 小鼠模型疾病活动指数 (DAI) 评分。Pharmacokinetic Analysis of BET BD2-IN-1 in Sprague Dawley Rats ModelparameterAUC(0?t) (ng?h/mL)C0 (ng/mL)T1/2 (h)CL (mL/kg/min)Vdss (L/kg)
iv(1 mg/kg)272 ± 7.2279 ± 781.5 ± 0.160 ± 2.06.6 ± 0.8
parameterAUC(0?t) (ng?h/mL)Cmax (ng/mL)T1/2 (h)Tmax (h)F (%)
po(10 mg/kg)78 ± 3420 ± 111.9 ± 0.22.7 ± 1.2 2.9 ± 1.2
Animal Model:Imiquimod (HY-B0180)-induced Psoriasis mouse model
Dosage:10 and 20 mg/kg
Administration:Intravenous injection (i.v.) ; Once daily for seven days
Result:Significantly alleviated the Imiquimod-induced skin lesions in a dose-dependent manner. Obviously reduced the enlarged spleen. Significantly decreased the expression of p-STAT3 and p-NF-κB in mouse skin tissues.
Animal Model:DSS (HY-116282C)-induced IBD mouse model
Dosage:10 and 20 mg/kg
Administration:Intravenous injection (i.v.) ; Once daily for seven days
Result:Effectively prevented colon shortening. Effectively alleviated the DSS-induced weight loss. Significantly alleviated the infiltration of inflammatory cells, areas of ulceration as well as loss of mucosal epithelium, and goblet cells caused by DSS.
体外研究：
BET BD2-IN-1 (500 nM) 能有效抑制 Th17 细胞分化，对 BD2 的选择性优于 BD1。BET BD2-IN-1 (4 nM) 在完整细胞中与 BRD4 BD2 结合，对 BRD4 BD2 具有稳定效应。
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