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: 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

461.79

C₁₉H₁₉Cl₃N₂O₃S

2227548-95-8

Solid

White to off-white

O=C(C1CCN(S(=O)(C2=CC(Cl)=CC(Cl)=C2)=O)CC1)NCC3=CC=C(Cl)C=C3

Room temperature in continental US; may vary elsewhere.

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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