AR-C141990 hydrochloride

Names

[ Name ]:
AR-C141990 hydrochloride

Biological Activity

[Description]:

AR-C141990 hydrochloride is a potent lactate transporters (monocarboxylate transporters; MCTs) inhibitor with pKi 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].

[Related Catalog]:

Signaling Pathways >> Membrane Transporter/Ion Channel >> Monocarboxylate Transporter

Research Areas >> Inflammation/Immunology

[Target]

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

[In Vitro]

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].

[In Vivo]

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].

[References]

[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.

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₆H₂₉ClN₄O₄S

[ Molecular Weight ]:
529.05

Safety Information

[ Hazard Codes ]:
Xi

Related Compounds

The content on this webpage is sourced from various professional data sources. If you have any questions or concerns regarding the content, please feel free to contact service1@chemsrc.com.