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

AR-C141990 hydrochloride has no significant activity against MCT-3 (pIC 50 <5) or MCT-4 (pIC 50 <5)[1]. AR-C141990 hydrochloride inhibits the uptake of [ 3 H]HOCPCA in oocytes expressing MCT1 or 2 in a concentration-dependent manner with IC 50 s of 0.21 μM and 2.32 μM, respectively[2].

AR-C141990 hydrochloride (10 mg/kg; SC) with a parallel decline in plasma concentrations with a half-life around 20 minutes in male NMRI mice (18-22 g)[2]. Application of the corresponding plasma concentrations of AR-C141990 hydrochloride (0.3-90 mg/kg) results in a concentration-dependent decrease in the B/P of HOCPCA with an EC 50 of 860 ng/ml[2]. AR-C141990 (100 mg/kg; s.c.) has a moderate prolongation of graft survival for 40 days in PVG rats that received DA cardiac transplants[1].