BI01383298 is a selective inhibitor of the sodium-citrate co-transporter (SLC13A5). BI01383298, has been shown as a highly potent inhibitor of human NaCT with an IC50 of 25–60 nM, significantly more potent than PF-06649298 (IC50, 0.4–10 µM). BI01383298 is a high-affinity inhibitor selective for human NaCT with no effect on mouse NaCT. The inhibition of human NaCT by BI01383298 is evident for the constitutively expressed transporter in HepG2 cells and for the ectopically expressed human NaCT in HEK293 cells. The IC50 is ∼100 nM, representing the highest potency among the NaCT inhibitors known to date.
| Molecular Weight | 445.34 |
| Formula | C19H19Cl2FN2O3S |
| CAS Number | 2227549-00-8 |
| Solubility (25°C) | DMSO 25 mg/mL |
| Storage | -20°C, protect from light, dry, sealed |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[2] Jeffrey M Peters. J Biol Chem. Flipping a citrate switch on liver cancer cells
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