| Description | SLC13A5-IN-1 is a selective inhibitor of sodium-citrate co-transporter (SLC13A5),completely blocks the uptake of 14C-citrate(IC50 : 0.022 μM in HepG2 cells). |
| In vitro | 在HepG2/14C-柠檬酸摄取试验中，SLC13A5-IN-1显示出0.022 μM的IC50值。HepG2细胞内源性地表达hSLC13A5转运蛋白，该转运蛋白负责柠檬酸进入这些细胞。SLC13A5-IN-1能完全阻断14C-柠檬酸的摄取，并且该信号可以被未标记的柠檬酸竞争。在重组hSLC3A5/14C-柠檬酸摄取试验中，SLC13A5-IN-1的IC50值为0.056 μM。而在重组人GlyT2/3H-甘氨酸摄取试验中，SLC13A5-IN-1的IC50值达到了100 μM。在该试验中使用的是稳定过表达人GlyT2受体的人胚肾293细胞，这些受体负责甘氨酸进入细胞。SLC13A5-IN-1能完全阻断3H-甘氨酸的摄取。 |
| Target activity | HepG2/14C-Citrate uptake:0.022 μM , Recombinant hSLC3A5/14C-Citrate Uptake:0.056 μM |
| molecular weight | 461.79 |
| Molecular formula | C19H19Cl3N2O3S |
| CAS | 2227548-95-8 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 5 mg/ml (10.83 mM), Sonication is recommended. |
| References | 1. Joerg Kley, et al. Sulfonamides as inhibitors of the uptake of extracellular citrate. Patent WO2018104220A1 |