RN486 

RN486 is a potent, selective and orally active Btk inhibitor with an IC₅₀ of 4.0 nM and a K_d of 0.31 nM. RN486 is less active for other kinases. RN486 can be used for rheumatoid arthritis and systemic lupus erythematosus research^[1][2][3].

IC50: 4.0 nM (Btk)^[1]
Kd: 0.31 nM (Btk)^[1]

RN486 blocks 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 nM), and B cell antigen receptor-induced expression of an activation marker, CD69, in B cells in whole blood (IC₅₀ = 21 nM)^[1].
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 is dose-dependently blocked by RN486^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

RN486 produces robust anti-inflammatory and bone-protective effects in mouse CIA and rat adjuvant-induced arthritis (AIA) models. In the AIA model, RN486 (1-30 mg/kg) inhibits both joint and systemic inflammation, reducing both paw swelling and inflammatory markers in the blood^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

606.69

C₃₅H₃₅FN₆O₃

1242156-23-5

Solid

Off-white to light yellow

O=C1C(NC2=CC=C(N3CCN(C)CC3)C=N2)=CC(C4=CC=CC(N5C=CC(C=C(C6CC6)C=C7F)=C7C5=O)=C4CO)=CN1C

Room temperature in continental US; may vary elsewhere.

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

• [1]. Xu D, et al. RN486, a selective Bruton's tyrosine kinase inhibitor, abrogates immune hypersensitivity responses and arthritis in rodents. J Pharmacol Exp Ther. 2012 Apr;341(1):90-103.  [Content Brief]

  [2]. Hsu J, et al. Bruton's Tyrosine Kinase mediates platelet receptor-induced generation of microparticles: a potential mechanism for amplification of inflammatory responses in rheumatoid arthritis synovial joints. Immunol Lett. 2013 Feb;150(1-2):97-104.  [Content Brief]

  [3]. Mina-Osorio P, et al. Suppression of glomerulonephritis in lupus-prone NZB × NZW mice by RN486, a selective inhibitor of Bruton's tyrosine kinase. Arthritis Rheum. 2013 Sep;65(9):2380-91.  [Content Brief]