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Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $106 | In Stock | |
5 mg | $263 | In Stock | |
10 mg | $396 | In Stock | |
25 mg | $752 | In Stock | |
50 mg | $1,090 | In Stock | |
100 mg | $1,670 | In Stock | |
1 mL x 10 mM (in DMSO) | $296 | In Stock |
Description | Tolebrutinib (PRN2246) is a potent, selective, orally active and brain-penetrant Bruton tyrosine kinase (BTK) inhibitor(IC50s of 0.4 and 0.7 nM in Ramos B cells and in HMC microglia cells, respectively). It exhibits efficacy in central nervous system immunity. Tolebrutinib can be used for the research of multiple sclerosis (MS). |
Targets&IC50 | BTK:0.4 nM (in Ramos B cells) , BTK:0.7 nM(in HMC microglia cell) |
In vitro | PRN2246 inhibits microglial FcγR activation through durable occupancy of BTK, with an IC50 of 157 nM.?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[1]. |
In vivo | PRN2246 produces dose-dependent protection from in myelin oligodendrocyte glycoprotein (MOG)-induced experimental autoimmune encephalomyelitis (EAE) model[1] |
Alias | PRN2246, SAR442168 |
Molecular Weight | 455.51 |
Formula | C26H25N5O3 |
Cas No. | 1971920-73-6 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 100 mg/mL (219.53 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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