Enpatoran (M5049) is a potentially "first-in-class" orally active Toll-like receptor (TLR) 7/8 inhibitor with IC50s of 11.1 nM and 24.1 nM in HEK293 cells. Enpatoran showed no activity against TLR3, TLR4 and TLR9. Enpatoran blocks both molecular synthesis ligand and natural endogenous RNA ligand. Enpatoran showed good pharmacokinetic characteristics in vivo. Enpatoran can be used in the study of congenital and adaptive autoimmune blocking.
| Molecular Weight | 320.31 |
| Formula | C16H15F3N4 |
| CAS Number | 2101938-42-3 |
| Solubility (25°C) | DMSO ≥ 20 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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