PF-06761281 (Compound 4a) is a potent and partially selective sodium-coupled citrate transporter protein (NaCT/SLC13A5) inhibitor with IC50 values of 0.51, 13.2, and 14.1 µM for NaCT, NaDC, and NaDC, respectively, and has the advantage of being orally active, reducing hepatic and renal uptake of citrate and plasma glucose concentration for metabolic diseases.

Selectivity over NaDC1/NaDC3:~13 μM, HEK293 cells:0.51 μM

PF-06761281 是NaCT抑制剂，在HEK293细胞中IC₅₀为0.51 μM，在人、小鼠和大鼠肝细胞中IC₅₀分别为0.74、0.21和0.12 μM，对NaDC1/NaDC3选择性高（IC₅₀约13 μM）。水溶性24 mM（pH 6.5），渗透性低（P_app = 0.3×10⁻⁶ cm/s），肝细胞清除率<7 μL/min/10⁶ cells[1]。