AR-C141990 hydrochloride 

AR-C141990 hydrochloride is a potent lactate transporters (monocarboxylate transporters; MCTs) inhibitor with pK_i values of 7.6, 6.6 for MCT-1 and MCT-2, respectively^[1]. AR-C141990 hydrochloride has immunosuppressive properties and inhibits graft versus host response^[2].

pKi: 7.6 (MCT-1) and 6.6 (MCT-2)^[1]

AR-C141990 hydrochloride has no significant activity against MCT-3 (pIC₅₀<5) or MCT-4 (pIC₅₀<5)^[1].
AR-C141990 hydrochloride inhibits the uptake of [³H]HOCPCA in oocytes expressing MCT1 or 2 in a concentration-dependent manner with IC₅₀s of 0.21 µM and 2.32 µM, respectively^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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 EC₅₀ 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

529.05

C₂₆H₂₉ClN₄O₄S

2250019-94-2

Solid

White to off-white

O=C1N(CC(C)C)C2=C(C(C(N3C[C@H](O)CC3)=O)=C(CC4=CC=NC5=CC=CC=C45)S2)C(N1C)=O.[H]Cl

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

• [1]. Clara Påhlman, et al. Immunosuppressive Properties of a Series of Novel Inhibitors of the Monocarboxylate Transporter MCT-1. Transpl Int. 2013 Jan;26(1):22-9.  [Content Brief]

  [2]. Louise Thiesen, et al. In Vitro and In Vivo Evidence for Active Brain Uptake of the GHB Analog HOCPCA by the Monocarboxylate Transporter Subtype 1. J Pharmacol Exp Ther. 2015 Aug;354(2):166-74.  [Content Brief]