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]. IC50 & Target: IC50: 0.022 μM (HepG2/¹⁴C-Citrate Uptake Assay); 0.056 μM (recombinant hSLC3A5/¹⁴C-Citrate Uptake Assay)^[1] In Vitro: 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].