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Enpatoran hydrochloride

Cat. No. M11461
Enpatoran hydrochloride Structure
Synonym:

M5049 hydrochloride

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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

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.

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 356.77
Formula C16H16ClF3N4
CAS Number 2101945-93-9
Purity >98%
Solubility DMSO ≥ 10 mg/mL
Storage -20°C , protect from light , dry , sealed
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