Catalog Number: 5658
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.
Background References
  1. Immunosuppressive properties of a series of novel inhibitors of the monocarboxylate transporter MCT-1.
    Påhlman et al.
    Transpl.Int., 2012;26:22
  2. In vitro and in vivo evidence for active brain uptake of the GHB analog HOCPCA by the monocarboxylate transporter subtype 1.
    Thiesen et al.
    J.Pharmacol.Exp.Ther., 2015;354:166
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