RN486 is a potently and selectively inhibitor. RN486 inhibited the Btk enzyme and displayed functional activities in human cell-based assays in multiple cell types. RN486 blocks Fcε receptor cross-linking-induced degranulation in mast cells (IC(50) = 2.9 nM), Fcγ receptor engagement-mediated tumor necrosis factor α production in monocytes (IC(50) = 7.0 nM), and B cell antigen receptor-induced expression of an activation marker, CD69, in B cells in whole blood (IC(50) = 21.0 nM). RN486 produced robust anti-inflammatory and bone-protective effects in mouse CIA and rat adjuvant-induced arthritis (AIA) models. In the AIA model, RN486 inhibited both joint and systemic inflammation either alone or in combination with methotrexate, reducing both paw swelling and inflammatory markers in the blood.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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.
RN486, a selective Bruton's tyrosine kinase inhibitor, abrogates immune hypersensitivity responses and arthritis in rodents.
Xu D, et al. J Pharmacol Exp Ther. 2012 Apr;341(1):90-103. PMID: 22228807.
|Related BTK Products|
Remibrutinib (LOU064) is a potent and highly selective covalent Inhibitor of Bruton's Tyrosine Kinase (BTK) with IC50 value of 1 nM.
Tolebrutinib, also known as SAR442168, is a Bruton tyrosine kinase (BTK) inhibitor, with IC50 values of 0.4 nM and 0.7 nM in Ramos B cells and HMC microglia cells, respectively.
Orelabrutinib is an orally active and irreversible inhibitor of Bruton's tyrosine kinase (BTK).
Zanubrutinib (BGB-3111) is a potent and highly selective small molecule inhibitor of Bruton's tyrosine kinase (BTK).
ARQ 531 is a potent reversible inhibitor of BTK (IC50 = 0.85 nM), exhibits potent antitumor activity in ibrutinib-resistant diffuse large B-cell lymphoma.
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