For research use only. Not for therapeutic Use.
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AR-C155858(cas 496791-37-8) is a novel inhibitor of the monocarboxylate transporters (MCTs) MCT1 and MCT2 (Ki values are 2.3 and <10 nM respectively); exhibits no activity at MCT4.<br />
Co-expression of exogenous embigin was without effect on either the expression of MCT1 or its inhibition by AR-C155858. In contrast, expression of active MCT2 at the plasma membrane of oocytes was significantly enhanced by co-expression of exogenous embigin. This additional transport activity was insensitive to inhibition by AR-C155858 unlike that by MCT2 expressed with endogenous basigin that was potently inhibited by AR-C155858. Derived values were 2.3+/-1.4 nM, 1.29+/-0.09 nmol per ml of packed cells and 12.2+/-1.1 s-1 respectively. When expressed in Xenopus laevis oocytes, MCT1 and MCT2 were potently inhibited by AR-C155858, whereas MCT4 was not. Inhibition of MCT1 was shown to be time-dependent, and the compound was also active when microinjected, suggesting that AR-C155858 probably enters the cell before binding to an intracellular site on MCT1.
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| Catalog Number | I003741 |
| CAS Number | 496791-37-8 |
| Synonyms | 6-[(3,5-dimethyl-1H-pyrazol-4-yl)methyl]-5-[(4S)-4-hydroxy-1,2-oxazolidine-2-carbonyl]-3-methyl-1-(2-methylpropyl)thieno[2,3-d]pyrimidine-2,4-dione |
| Molecular Formula | C21H27N5O5S |
| Purity | ≥95% |
| Target | Monocarboxylate Transporter |
| Solubility | in DMSO > 10 mM |
| Storage | Store at -20°C |
| IC50 | 2.3/<10 nM (Ki, MCT1/2) |
| IUPAC Name | 6-[(3,5-dimethyl-1H-pyrazol-4-yl)methyl]-5-[(4S)-4-hydroxy-1,2-oxazolidine-2-carbonyl]-3-methyl-1-(2-methylpropyl)thieno[2,3-d]pyrimidine-2,4-dione |
| InChI | InChI=1S/C21H27N5O5S/c1-10(2)7-25-20-17(18(28)24(5)21(25)30)16(19(29)26-8-13(27)9-31-26)15(32-20)6-14-11(3)22-23-12(14)4/h10,13,27H,6-9H2,1-5H3,(H,22,23)/t13-/m0/s1 |
| InChIKey | ISIVOJWVBJIOFM-ZDUSSCGKSA-N |
| SMILES | CC1=C(C(=NN1)C)CC2=C(C3=C(S2)N(C(=O)N(C3=O)C)CC(C)C)C(=O)N4CC(CO4)O |
| Reference | 1:Identification of key binding site residues of MCT1 for AR-C155858 reveals the molecular basis of its isoform selectivity. Nancolas B, Sessions RB, Halestrap AP.Biochem J. 2015 Apr 1;467(1):192. No abstract available. PMID: 25793420 <br /> |
