Cat. No. Name Size Price Add Cart
KI2062AR-C1558585 mg$829.4
AR-C15585810 mg$1372.8
AR-C15585825 mg$2431

Chemical Characteristic

Product NameAR-C155858
SynonymsAR-C 155858
CAS No.496791-37-8
Molecular Weight 461.5
FormulaC21H27N5O5S
Chemical Name(s)-6-((3,5-dimethyl-1h-pyrazol-4-yl)methyl)-5-((4-hydroxyisoxazolidin-2-yl)carbonyl)-1-isobutyl-3-methylthieno(2,3-d)pyrimidine-2,4(1h,3h)-dione
Smilesc1(=O)n(c2c(c(=O)n1C)c(c(s2)Cc1c(n[nH]c1C)C)C(=O)N1OC[C@H](C1)O)CC(C)C
Chemical Structure

Biological activities

AR-C155858 is a potent monocarboxylate transporters (MCTs) inhibitor. AR-C155858 selectively inhibits MCT1 and MCT2 with Ki values of 2.3 and significantly less than 10 nM, respectively. However, MCT4 is not sensitive to inhibition by AR-C155858. In vitro, AR-C155858 time- and dose-dependently inhibits MCT1 expression in Xenopus oocytes.[1] Moreover, MCT2 to inhibition by AR-C155858 is desensitized by co-expression of embigin.[2]

Protocols

In vitro: Prior to use, AR-C155858 is dissolved in dimethyl sulfoxide (DMSO).[3]

References

[1] Ovens MJ, et al. The inhibition of monocarboxylate transporter 2 (MCT2) by AR-C155858 is modulated by the associated ancillary protein. Biochem J. 2010, 431(2): 217-225.
[2] Ovens MJ, et al. AR-C155858 is a potent inhibitor of monocarboxylate transporters MCT1 and MCT2 that binds to an intracellular site involving transmembrane helices 7-10. Biochem J. 2010, 425(3): 523-530.
[3] P?hlman C, et al. Immunosuppressive properties of a series of novel inhibitors of the monocarboxylate transporter MCT-1. Transpl Int. 2013, 26(1): 22-29.

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