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    RN486
    RN486

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0648
    CAS #: 1242156-23-5Purity ≥98%

    Description: RN486 (RN-486) is a novel, potent, reversible and selective BTK (Bruton's tyrosine kinase) inhibitor with potential anti-inflammatory activity. It inhibits BTK with an IC50 of 4 nM. RN486 exhibits strong in vivo anti-inflammatory and bone-protective effects in mouse CIA and rat adjuvant-induced arthritis (AIA) models. In the AIA model, RN486 inhibits both joint and systemic inflammation either alone or in combination with methotrexate, reducing both paw swelling and inflammatory markers in the blood.

    References: J Pharmacol Exp Ther. 2012 Apr;341(1):90-103.

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    Molecular Weight (MW)606.69
    FormulaC35H35FN6O3
    CAS No.1242156-23-5
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 62 mg/mL (102.2 mM)
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Solubility (In vivo)5% DMSO+30% PEG 300+10% Tween 80+ddH2O: 5mg/mL
    SynonymsRN-486; RN 486; RN486;  

    Chemical Name: 6-cyclopropyl-8-fluoro-2-(2-hydroxymethyl-3-{1-methyl-5-[5-(4-methyl-piperazin-1-yl)-pyridin-2-ylamino]-6-oxo-1,6-dihydro-pyridin-3-yl}-phenyl)-2H-isoquinolin-1-one

    InChi Key: ZTUJNJAKTLHBEX-UHFFFAOYSA-N

    InChi Code: InChI=1S/C35H35FN6O3/c1-39-12-14-41(15-13-39)26-8-9-32(37-19-26)38-30-18-25(20-40(2)34(30)44)27-4-3-5-31(28(27)21-43)42-11-10-23-16-24(22-6-7-22)17-29(36)33(23)35(42)45/h3-5,8-11,16-20,22,43H,6-7,12-15,21H2,1-2H3,(H,37,38)

    SMILES Code: O=C1N(C2=CC=CC(C(C=C3NC4=NC=C(N5CCN(C)CC5)C=C4)=CN(C)C3=O)=C2CO)C=CC6=C1C(F)=CC(C7CC7)=C6


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    In Vitro

    In vitro activity: RN486 not only potently and selectively inhibits the Btk enzyme, but also displays functional activities in human cell-based assays in multiple cell types, blocking Fcε receptor cross-linking-induced degranulation in mast cells (IC50 = 2.9 nM), Fcγ receptor engagement-mediated tumor necrosis factor α production in monocytes (IC50 = 7.0 nM), and B cell antigen receptor-induced expression of an activation marker, CD69, in B cells in whole blood (IC50 = 21.0 nM). RN486 is able to block the signaling of BCR as demonstrated by a marked inhibition of phosphorylation of both Btk and PLCγ2 in B cells. RN486 displays a selective B cell inhibitory profile in BioMAP Systems.


    Kinase Assay: RN486 is a novel, potent and selective BTK inhibitor with IC50 of 4 nM. RN486 not only potently and selectively inhibited the Btk enzyme, but also displayed functional activities in human cell-based assays in multiple cell types, blocking 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). 


    Cell Assay: In a co-culture system consisting of human primary synovial FLS and activated human platelets, convulxin stimulation resulted in elevated production of pro-inflammatory cytokines, IL-6 and IL-8, an effect which was dose-dependently blocked by RN486.

    In VivoRN486 displays similar functional activities in rodent models, effectively preventing type I and type III hypersensitivity responses. More importantly, RN486 produces robust anti-inflammatory and bone-protective effects in mouse CIA and rat adjuvant-induced arthritis (AIA) models. In the AIA model, RN486 inhibits both joint and systemic inflammation either alone or in combination with methotrexate, reducing both paw swelling and inflammatory markers in the blood.
    Animal modelRodent models
    Formulation & DosageN/A 
    ReferencesJ Pharmacol Exp Ther. 2012 Apr;341(1):90-103.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    RN486

    Inhibitory effect of RN486 on the effector phase of immune arthritis in mice. J Pharmacol Exp Ther. 2012 Apr;341(1):90-103.

    RN486

    Anti-inflammatory and disease-modifying effects of RN486 in the rat AIA model. J Pharmacol Exp Ther. 2012 Apr;341(1):90-103.

    RN486

    Additive inhibitory effects of RN486 and MTX on inflammation and bone erosions in the rat AIA model. J Pharmacol Exp Ther. 2012 Apr;341(1):90-103.


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