产品
编 号:F237886
分子式:C15H22N4O2
分子量:290.36
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10mM*1mL in DMSO
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1mg
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5mg
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10mg
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生物活性:
KDM5A-IN-1 is a potent, orally bioavailable pan-histone lysine demethylases 5 (KDM5) inhibitor with IC50s of 45 nM, 56 nM and 55 nM for KDM5A, KDM5B and KDM5C, respectively, and with an EC50 value of 960 nM for PC9 H3K4Me3. KDM5A-IN-1 is significantly less potent against other KDM5B enzymes (1A, 2B, 3B, 4C, 6A, 7B).

体内研究:
KDM5A-IN-1(化合物50,5 mg/kg;口服;雌性CD-1小鼠) 对小鼠的清除率中等 (28 mL/min/kg),具有良好的口服生物利用度(F% 34),小鼠血浆蛋白结合明显低(40%),t1/2为0.4小时。Animal Model:Female CD-1 mice
Dosage:5 mg/kg
Administration:Oral administration (Pharmacokinetic study)
Result:Moderate clearance (28 mL/min/kg) in mice with good oral bioavailability (F% 34), and showed remarkably low plasma protein binding in mice (40%).
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