SLC13A5-IN-1

• CAT Number: I045992
• CAS Number: 2227548-95-8
• Molecular Formula: C19H19Cl3N2O3S
• Molecular Weight: 461.79
• Purity: ≥95%
• Synonyms: N-[(4-chlorophenyl)methyl]-1-(3,5-dichlorophenyl)sulfonylpiperidine-4-carboxamide
• InChI: InChI=1S/C19H19Cl3N2O3S/c20-15-3-1-13(2-4-15)12-23-19(25)14-5-7-24(8-6-14)28(26,27)18-10-16(21)9-17(22)11-18/h1-4,9-11,14H,5-8,12H2,(H,23,25)
• InChIKey: NPEIWANTVUZMJV-UHFFFAOYSA-N
• SMILES: C1CN(CCC1C(=O)NCC2=CC=C(C=C2)Cl)S(=O)(=O)C3=CC(=CC(=C3)Cl)Cl

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].
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].

Reference

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