TYK2-IN-12, an orally active, potent, and selective inhibitor of TYK2 (tyrosine kinase 2), with a Ki of 0.51 nM, inhibits IL-12-induced IFNγ, with IC50 values of 2.7 and 7.0 μM in human and mouse whole blood, respectively. It serves as a valuable tool for psoriasis research[1].
体内研究
Administered orally at doses ranging from 0 to 100 mg/kg daily for 10 days, TYK2-IN-12 dose-dependently reduces immune responses[1].
TYK2-IN-12, administered once at doses of 3 mg/kg (intravenous) and 10 mg/kg (oral), demonstrates moderate clearance and volumes of distribution, with moderate to good oral absorption[1].
Pharmacokinetic Parameters of TYK2-IN-12 in male C57Bl/6 mice and male Sprague-Dawley rats[1].
体外研究
TYK2-IN-12 exhibits 90, 43, and 13-fold selectivity over JAK1, JAK2, and JAK3, respectively[1].
With excellent selectivity over hERG (IC50 > 30 μM) and a panel of 10 cytochrome P450 enzymes (IC50s > 30 μM against CYP450s 3A4, 3D6, 2C9, 2C8, 1A2, 2A6, 2B6, 2C19, 2E1, and 3A5), TYK2-IN-12 displays favorable selectivity profiles[1].
TYK2-IN-12 exhibits cell-based potency and selectivity in human PBMCs by blocking IL-12-induced phospho-STAT4, GM-CSF-induced phospho-STAT5, and IL-2-induced phospho-STAT5, with IC50 values of 0.10 μM, 4.1 μM, and 0.25 μM, respectively[1].
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