GNE-9822 is a potent, orally active and selective ITK inhibitor with a K i value of 0.7 nM. GNE-9822 has good ADME properties. GNE-9822 can be used in research of asthma.
In Vitro
GNE-9822 (compound 28) inhibits the phosphorylation of PLCγ with an IC 50 value of 55 nM. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
GNE-9822 (compound 28; po and iv; 1 and 5 mg/kg) has good bioavailability and halflives observed in mouse and rats . MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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: 1.19 species route dose volume (mL/kg) dose (mg/kg) C max (μM) AUC (μM·h) Cl (mL/min/kg) T 1/2 (h) V ss (L/kg) %F mouse (BALB/c) IV 1.0 1.0 1.5 40 2.9 10 mouse (BALB/c) PO 5.0 50 3.8 2.7 36 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: 1.19 species route dose volume (mL/kg) dose (mg/kg) C max (μM) AUC (μM·h) Cl (mL/min/kg) T 1/2 (h) V ss (L/kg) %F rat (Sprague-Dawley IV 1.0 1.0 0.6 70 3.0 14 rat (Sprague-Dawley PO 2.0 5.0 0.2 1.1 40
