Bioactivity | PF-06761281 (Compound 4a) is a potent, orally active, partial selective sodium-coupled citrate transporter (NaCT or SLC13A5) inhibitor with IC50 values of 0.51, 13.2 and 14.1 µM against HEKNaCT, HEKNaDC1 and HEKNaDC3, respectively[1]. |
Target | IC50: 0.51 µM (HEKNaCT), 13.2 µM (HEKNaDC1), 14.1 µM (HEKNaDC3) |
Invitro | PF-06761281 (Compound 4a) inhibits citrate uptake with IC50 values of 0.12, 0.21 and 0.74 µM in rat, mouse and human Heps[1]. |
Name | PF-06761281 |
CAS | 1854061-19-0 |
Formula | C13H17NO6 |
Molar Mass | 283.28 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
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. |