AR-C 141990 hydrochloride

Cat. No. 5658new

AR-C 141990 hydrochloride C26H28N4O4S.HCl

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Chemical Name: 5-[[(3R)-3-Hydroxy-1-pyrrolidinyl]carbonyl]-3-methyl-1-(2-methylpropyl)-6-(4-quinolinylmethyl)thieno[2,3-d]pyrimidine-2,4(1H,3H)-dione

Biological Activity

Monocarboxylate transporter (MCT1) inhibitor (pKi = 7.6. Exhibits approximately 10-fold selectivity for MCT1 over MCT2 and no significant activity against MCT3 or 4. Inhibits graft versus host response and prolongs cardiac graft survival in a rat model. Immunosuppressant. Also inhibits brain penetration of GHB analog HOCPCA.

Technical Data

M.Wt:
529.05
Formula:
C26H28N4O4S.HCl
Solubility:
Soluble to 100 mM in water and to 100 mM in DMSO
Purity:
>98 %
Storage:
Store at -20°C

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Product Datasheet / Safety Datasheet

References are publications that support the products' biological activity.

Thiesen et al (2015) 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. 354 166. PMID: 25986445.

Påhlman et al (2012) Immunosuppressive properties of a series of novel inhibitors of the monocarboxylate transporter MCT-1. Transpl.Int. 26 22. PMID: 23137339.

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Keywords: AR-C 141990 hydrochloride, supplier, AR-C141990, HCl, monocarboxylate, transporter, 1, MCT1, immunosuppressant, graft, versus, host, GvH, transplant, Tocris Bioscience, Monocarboxylate Transporter Inhibitor products

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