OAT-2068

OAT-2068 is a selective, high activity and orally active inhibitor of mouse chitotriosidase (mCHIT1) (IC₅₀=29 nM) and displays 143-fold selectivity over m AMCase (IC₅₀=4170 nM). OAT-2068 displays a good pharmacokinetic profile and is an ideal tool to study the role of CHIT1 in biological systems, including animal models of human diseases^[1]. IC50 & Target:IC50: 29 nM (mCHIT1); 4200 nM (mAMCase)
IC50: 67 nM (hCHIT1); 1300 nM (hAMCase)^[2] In Vitro: OAT-2068 is a potent inhibitor developed for mAMCase (IC₅₀=4200 nM) and mCHIT1(IC₅₀=29 nM), which also displays activity toward hAMCase (IC₅₀=67 nM) and hCHIT1 (IC₅₀=1300 nM), it exhibits off-target activity toward the human ether-a-go-go-related gene (hERG)(hERG IC₅₀=2.4 μM)^[2]. In Vivo: OAT-2068 (intravenous injection; 3 mg/kg; single dose) displays a favorable pharmacokinetic profile, showing moderate plasma clearance (1.71 mg*kg/L),good volume of distribution (4.6 L/h/kg), and T_1/2 (2.87 h) in female BALB/c mice^[1].
OAT-2068 (oral administartion; 10 mg/kg; single dose) displays a favorable pharmacokinetic profile,it is rapidly absorbed with T_max 0.5 h and exhibited a high bioavailability of 61%, the T_1/2 and the plasma clearance are 2.83 hours and 3.57 mg*kg/L, respectively^[1].