slc13a5

SLC13A5-IN-1 is a selective inhibitor of the sodium-citrate co-transporter (SLC13A5) that completely blocks the uptake of 14C-citrate, with an IC50 of 0.022 μM in HepG2 cells.

BI 01383298 is a selective inhibitor of the sodium-citrate co-transporter (SLC13A5).

LBA-3, a selective and orally active inhibitor of the sodium-coupled citrate transporter SLC13A5, exhibits an IC50 of 67 nM. This compound effectively reduces triglyceride and total cholesterol levels in both oleic and palmitic acid (OPA)-stimulated AML12 cells and PCN-stimulated primary mouse hepatocytes, as well as in mouse models, without showing detectable toxicity. Additionally, LBA-3 is permeable to the blood-brain barrier [1].

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.