产品
编 号：F756621
分子式：C26H34N4O7S
分子量：546.64
分子式：C26H34N4O7S
分子量：546.64
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CAS No: 2885162-99-0
产品详情
生物活性：
I-BET282E is a pan-inhibitor of all eight BET bromodomains, and selectivity over other representative bromodomain-containing proteins. I-BET282E shows pIC50s ranging 6.4-7.7 for BRD2 (BD1/BD2), BRD2 (BD1/BD), BRD3 (BD1/BD), and BRD4 (BD1/BD).
体内研究：
I-BET282E (Male CD1 Mice; 3 mg/kg-p.o.; 1 mg/kg-i.v.) treatment shows the Clb, LBF, Vss, t1/2 (i.v.), and F values of 23 mL/min/kg, 19%, 1.9 L/kg, and 51%, respectively.I-BET282E (Male Wistar Han Rats; 1 mg/kg; p.o.) treatment shows the AUC0-t, Cmax and Tmax values of 467 ng h/mL, 125 ng/mL, and 1 hour, respectively.
体外研究：
I-BET282E has a weak inhibition of the hERG potassium ion channel (pIC50 4.4-5.1 in a variety of assay formats). I-BET282E shows a low potential to inhibit CYP proteins in vitro, with no evidence of time-dependent inhibition of 2D6 or 3A4.
I-BET282E is a pan-inhibitor of all eight BET bromodomains, and selectivity over other representative bromodomain-containing proteins. I-BET282E shows pIC50s ranging 6.4-7.7 for BRD2 (BD1/BD2), BRD2 (BD1/BD), BRD3 (BD1/BD), and BRD4 (BD1/BD).
体内研究：
I-BET282E (Male CD1 Mice; 3 mg/kg-p.o.; 1 mg/kg-i.v.) treatment shows the Clb, LBF, Vss, t1/2 (i.v.), and F values of 23 mL/min/kg, 19%, 1.9 L/kg, and 51%, respectively.I-BET282E (Male Wistar Han Rats; 1 mg/kg; p.o.) treatment shows the AUC0-t, Cmax and Tmax values of 467 ng h/mL, 125 ng/mL, and 1 hour, respectively.
体外研究：
I-BET282E has a weak inhibition of the hERG potassium ion channel (pIC50 4.4-5.1 in a variety of assay formats). I-BET282E shows a low potential to inhibit CYP proteins in vitro, with no evidence of time-dependent inhibition of 2D6 or 3A4.
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