For research use only. Not for therapeutic Use.
PF-06649298 is a sodium-coupled citrate transporter (NaCT or SLC13A5) inhibitor. PF-06649298 specifically interacts with NaCT with an IC50 value of 16.2 μM to inhibits the transport of citrate in human hepatocytes. PF-06649298 can be used for the research of regulating glucose metabolism and lipid metabolism[1][2].
PF-06649298 (0-100 μM; 30 min) inhibits citrate uptaken in cells[1].
PF-06649298 (250 mg/kg; p.o. twice a day; for 21 days) reverses glucose intolerance of high fat diet (HFD) mice[2].
| Catalog Number | I042961 |
| CAS Number | 1854061-16-7 |
| Synonyms | (2R)-2-[2-(4-tert-butylphenyl)ethyl]-2-hydroxybutanedioic acid |
| Molecular Formula | C16H22O5 |
| Purity | ≥95% |
| InChI | InChI=1S/C16H22O5/c1-15(2,3)12-6-4-11(5-7-12)8-9-16(21,14(19)20)10-13(17)18/h4-7,21H,8-10H2,1-3H3,(H,17,18)(H,19,20)/t16-/m1/s1 |
| InChIKey | QNFWRHKLBLSSPB-MRXNPFEDSA-N |
| SMILES | CC(C)(C)C1=CC=C(C=C1)CCC(CC(=O)O)(C(=O)O)O |
| Reference | [1]. Huard K, et al. Optimization of a Dicarboxylic Series for in Vivo Inhibition of Citrate Transport by the Solute Carrier 13 (SLC13) Family. J Med Chem. 2016 Feb 11;59(3):1165-75. [2]. Huard K, et al. Discovery and characterization of novel inhibitors of the sodium-coupled citrate transporter (NaCT or SLC13A5). Sci Rep. 2015 Dec 1;5:17391. |
