AR-C141990 hydrochloride is a potent inhibitor of lactate transporters known as monocarboxylate transporters (MCTs), with pK i values of 7.6 and 6.6 for MCT-1 and MCT-2, respectively. This compound also exhibits immunosuppressive properties and effectively inhibits the graft versus host response.

AR-C141990 hydrochloride exhibits negligible activity against MCT-3 (pIC 50 <5) and MCT-4 (pIC 50 <5)[1]. However, it effectively inhibits the uptake of [3H]HOCPCA in oocytes expressing MCT1 or 2, demonstrating concentration-dependent inhibition with IC50 values of 0.21 μM for MCT1 and 2.32 μM for MCT2, respectively[2].

Administering AR-C141990 hydrochloride (10 mg/kg; SC) to male NMRI mice (18-22 g) resulted in a rapid decrease in its plasma concentrations, exhibiting a half-life of approximately 20 minutes[2]. The plasma levels of AR-C141990 hydrochloride (0.3-90 mg/kg) were found to reduce the B/P of HOCPCA in a concentration-dependent manner, with an EC50 of 860 ng/ml[2]. Furthermore, a dose of AR-C141990 (100 mg/kg; s.c.) was observed to moderately extend the survival of grafts to 40 days in PVG rats that underwent DA cardiac transplants[1].