ERG240 is a selective inhibitor of branched-chain aminotransferase 1 (BCAT1) with an IC50 of 0.1-1nM. ERG240 leads to decreased oxygen consumption and glycolysis through the down regulation of IRG1 expression, which leads to decrease itaconate production in human macrophages. EGR240 can be used for the research of cancer, rheumatoid arthritis, and bone disease.
| CAS Number | 1415683-79-2 |
| Solubility (25°C) | DMSO 60 mg/mL Water 60 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.
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