AR-C141990 hydrochloride_product_DataBase

Bioactivity	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].
Target	pKi: 7.6 (MCT-1) and 6.6 (MCT-2)
Invitro	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].
Name	AR-C141990 hydrochloride
CAS	2250019-94-2
Formula	C26H29ClN4O4S
Molar Mass	529.05
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[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.

PeptideDB

AR-C141990 hydrochloride

CAS: 2250019-94-2 F: C26H29ClN4O4S W: 529.05