Tolebrutinib| ChemScene

Tolebrutinib (SAR442168) is a potent, selective, orally active and brain-penetrant inhibitor of Bruton tyrosine kinase (BTK), with IC50s of 0.4 and 0.7 nM in Ramos B cells and in HMC microglia cells, respectively. Tolebrutinib exhibits efficacy in central nervous system immunity. Tolebrutinib can be used for the research of multiple sclerosis (MS)[2].IC50 & Target: IC50: 0.7 nM (BTK; in HMC microglia cells)[2]In Vitro: PRN2246 blocks the BCR-mediated activation (IC50=10 nM) and Fc receptor activation (IC50=166 and 9.6 nM for FcεR and FcγR, repectively) of immune cells[2].
PRN2246 inhibits microglial FcγR activation through durable occupancy of BTK, with an IC50 of 157 nM[2].In Vivo: PRN2246 (1-5 mg/kg; p.o. q.d. for 28 d) produces dose-dependent protection from in myelin oligodendrocyte glycoprotein (MOG)-induced experimental autoimmune encephalomyelitis (EAE) model[2].

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Trivial name Tolebrutinib
Catalog Number CS-0119132
Alternative Name(s) SAR442168; PRN2246
Molecular Formula 455.51
CAS# 1971920-73-6
Purity >98%
Condensed Formula C26H25N5O3
Size 50mg
Supplier Page www.chemscene.com/1971920-73-6.html