Enpatoran, also known as M5049, is a novel potent and selective TLR7/8 inhibitor for treatment of autoimmunity. M5049 showed potent and selective activity in a range of cellular assays for inhibition of TLR7/8 and block synthetic ligands and natural endogenous RNA ligands such as microRNA and Alu RNA. M5049 was found to be potent in vivo as TLR7/8 inhibition efficaciously treated disease in several murine lupus models. M5049 had greater potency in disease models than expected based on its in vitro potency and pharmacokinetic/pharmacodynamic properties. M5049 may be efficacious in treating autoimmunity and has the potential to provide benefit to a variety of patients with varying disease pathogenesis.
Cat.No
DC75622
Name
Enpatoran free base
Chemical Properties
CAS
2101938-42-3
Formula
C16H15F3N4
MW
320.319
Storage
2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
References
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