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编 号:F185147
分子式:C24H32N6O
分子量:420.55
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1mg
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5mg
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10mg
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生物活性:
GNE-9822 is a potent, orally active and selective ITK inhibitor with a Ki value of 0.7 nM, and an EC50 value of 354.5 nM. GNE-9822 has good ADME properties. GNE-9822 can be used in research of asthma.

体内研究:
GNE-9822 (compound 28; po and iv; 1 and 5 mg/kg) 在小鼠和大鼠中观察到良好的生物利用度和半衰期。Animal Model:BALB/c mouse and Sprague-Dawley rats
Dosage:1 and 5 mg/kg
Administration:po (5 mg/kg) and iv (1 mg/kg)
Result:1.19speciesroutedose volume (mL/kg)dose (mg/kg)Cmax (μM)AUC (μM·h)Cl (mL/min/kg)T1/2 (h)Vss (L/kg)%F
mouse (BALB/c)IV1.01.01.5402.910
mouse (BALB/c)PO5.0503.82.736

Animal Model:BALB/c mouse and Sprague-Dawley rats
Dosage:1 and 5 mg/kg
Administration:po (5 mg/kg) and iv (1 mg/kg)
Result:1.19speciesroutedose volume (mL/kg)dose (mg/kg)Cmax (μM)AUC (μM·h)Cl (mL/min/kg)T1/2 (h)Vss (L/kg)%F
rat (Sprague-DawleyIV1.01.00.6703.014
rat (Sprague-DawleyPO2.05.00.21.140


体外研究:
GNE-9822 (compound 28) 抑制 PLCγ 的磷酸化,IC50 值为 55 nM。
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