BTK inhibitor 18 is a potent, selective,orally active and covalent Btk inhibitor with a IC₅₀ of 142 nM. BTK inhibitor 18 has anti-inflammatory activities.

BTK inhibitor 18 (Compound 27) irreversibly inhibits BTK by targeting a noncatalytic cysteine residue (Cys481) for covalent bond formation.
BTK inhibitor 18 (Compound 27) inhibits anti-IgM-induced activation of B cells in human whole blood with an IC₅₀ of 84 nM.
BTK inhibitor 18 (Compound 27) also inhibits BMX, LCK, ErbB4, TEC, and TXK kinases with IC₅₀ values of 129 nM, 130 nM, 377 nM, 409 nM, 1770 nM, respectively.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

BTK inhibitor 18 (Compound 27; 1-30 mg/kg; oral administration; once a day; for 7 days) treatment shows dose-dependent efficacy at reducing joint inflammation in a rat collagen-induced arthritis model.
The IV and PO pharmacokinetics of BTK inhibitor 18 (Compound 27) are investigated in nonfasted rats (1 and 5 mg/kg IV and PO) and fasted dogs (0.5 and 2.5 mg/kg IV and PO). IV pharmacokinetics are characterized by moderate clearance in rat and low clearance in dog, a moderate volume of distribution, and a short plasma half-life across both species (T_1/2 of 0.3 h and 1.9 h for rat and dog, respectively). The oral bioavailability is 30% and 68% in rat and dog, respectively.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

BTK inhibitor 18 (Compound 27; 1-30 mg/kg; oral administration; once a day; for 7 days) treatment shows dose-dependent efficacy at reducing joint inflammation in a rat collagen-induced arthritis model.
The IV and PO pharmacokinetics of BTK inhibitor 18 (Compound 27) are investigated in nonfasted rats (1 and 5 mg/kg IV and PO) and fasted dogs (0.5 and 2.5 mg/kg IV and PO). IV pharmacokinetics are characterized by moderate clearance in rat and low clearance in dog, a moderate volume of distribution, and a short plasma half-life across both species (T_1/2 of 0.3 h and 1.9 h for rat and dog, respectively). The oral bioavailability is 30% and 68% in rat and dog, respectively.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

• . Mark S Tichenor, et al. Discovery of a Potent and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase with Oral Anti-Inflammatory Activity. ACS Med Chem Lett. 2021 Apr 5;12(5):782-790.  [Content Brief]