SLC13A5-IN-1

SLC13A5-IN-1 is a selective sodium-citrate co-transporter (SLC13A5) inhibitor. SLC13A5-IN-1 completely blocks the uptake of 14C-citrate with an IC50 value of 0.022 μM in HepG2 cells. SLC13A5-IN-1 has the potential for the treatment of metabolic and/or cardiovascular diseases. SLC13A5-IN-1 is extracted from patent WO2018104220A1, Compound I-5[1].

Signaling Pathways >> Membrane Transporter/Ion Channel >> Sodium Channel

Research Areas >> Cardiovascular Disease

Research Areas >> Metabolic Disease

IC50: 0.022 μM (HepG2/14C-Citrate Uptake Assay); 0.056 μM (recombinant hSLC3A5/14C-Citrate Uptake Assay)[1]

SLC13A5-IN-1 exhibits an IC50 of 0.022 μM in HepG2/14C-Citrate Uptake Assay. HepG2 cells endogenously express hSLC13A5 transporter which is responsible for the uptake of citrate into these cells. Uptake of 14C-citrate can be completely blocked by SLC13A5-IN-1 and the signal can be competed with unlabelled citrate. T[1]. SLC13A5-IN-1 exhibits an IC50 of 0.056 μM in recombinant hSLC3A5/14C-Citrate Uptake Assay[1]. SLC13A5-IN-1 exhibits an IC50 of 100 μM in recombinant Human GlyT2/3H-Glycine Uptake Assay. The human embryonic kidney 293 cells are used that stably over-express the human GlyT2 receptor which is responsible for the uptake of glycine into these cells. Uptake of 3H-glycine can be completely blocked by SLC13A5-IN-1[1].

[1]. Joerg Kley, et al. Sulfonamides as inhibitors of the uptake of extracellular citrate. Patent WO2018104220A1