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Enpatoran

Cat. No. M11434
Enpatoran Structure
Synonym:

M5049

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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

Enpatoran (M5049) is a potent and orally active tlR7/8 inhibitor with IC50s of 11.1 nM and 24.1 nM in HEK293 cells, respectively. Enpatoran has no activity on TLR3, TLR4 and TLR9. Enpatoran blocks the synthesis of ligands and natural endogenous RNA ligands. Enpatoran showed good pharmacokinetic properties in vivo. Enpatoran can be used to study congenital and adaptive autoimmune blockade.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 320.31
Formula C16H15F3N4
CAS Number 2101938-42-3
Purity >99%
Solubility DMSO ≥ 20 mg/mL
Storage -20°C , protect from light , dry , sealed
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