Enpatoran (M5049) Hydrochloride is a potent and orally active inhibitor of TLR7/8, with IC50s of 11.1 nM and 24.1 nM in HEK293 cells. Enpatoran Hydrochloride had no activity on TLR3, TLR4 and TLR9. Enpatoran hydrochloride blocks the synthesis of ligands and natural endogenous RNA ligands. Enpatoran Hydrochloride showed good pharmacokinetic properties in vivo. Enpatoran Hydrochloride can be used in the study of congenital and adaptive autoimmune blockade.
Molecular Weight | 356.77 |
Formula | C16H16ClF3N4 |
CAS Number | 2101945-93-9 |
Solubility (25°C) | DMSO ≥ 10 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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