LKT Labs

Biochemicals for Life Science Research

RN-486

RN-486

Product ID R5212
Cas No. 1242156-23-5
Purity ≥98%
Product Unit SizeCostQuantityStock
1 mg $363.00 In stock
5 mg $549.00 In stock
Bulk Quote

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Description

RN-486 is an inhibitor of Bruton’s tyrosine kinase (Btk) that is currently in development as a potential treatment for rheumatoid arthritis; it exhibits anti-inflammatory, nephroprotective, and immunosuppressive activities. RN-486 decreases production of IL-6 and expression of IL-8, TNF, MMP1, and MMP10 in synovial tissue. In animal models of systemic lupus erythmatosus (SLE), RN-486 inhibits B-cell activation and anti-double-stranded DNA IgG production, suppressing progression of glomerulonephritis. In other animal models, this compound inhibits mast cell degranulation, preventing type I and III hypersensitivity responses and limiting joint and systemic inflammation. RN-486 also decreases TLR-9 signaling and cytokine production.

Product Info

Cas No.

1242156-23-5
Purity

≥98%
Formula

C35H35FN6O3
Formula Wt.

606.69
IUPAC Name

6-Cyclopropyl-8-fluoro-2-[2-(hydroxymethyl)-3-(1-methyl-5-{[5-(4-methyl-1-piperazinyl)-2-pyridinyl]amino}-6-oxo-1,6-dihydro-3-pyridinyl)phenyl]-1(2H)-isoquinolinone
Synonym

RN486
Solubility

DMSO: 24 mg/mL
Appearance

White to off white powder

Shipping and Storage

Store Temp

-20°C
Ship Temp

Ambient

Downloads

MSDS

R5212 MSDS PDF
Info Sheet

R5212 Info Sheet PDF

References

Zhao X, Huang W, Wang Y, et al. Discovery of novel Bruton's tyrosine kinase (BTK) inhibitors bearing a pyrrolo[2,3-d]pyrimidine scaffold. Bioorg Med Chem. 2015 Feb 15;23(4):891-901. PMID: 25596757.

Hartkamp LM, Fine JS, van Es IE, et al. Btk inhibition suppresses agonist-induced human macrophage activation and inflammatory gene expression in RA synovial tissue explants. Ann Rheum Dis. 2014 Apr 24. [Epub ahead of print]. PMID: 24764451.

Wang J, Lau KY, Jung J, et al. Bruton's tyrosine kinase regulates TLR9 but not TLR7 signaling in human plasmacytoid dendritic cells. Eur J Immunol. 2014 Apr;44(4):1130-6. PMID: 24375473.

Xu D, Kim Y, Postelnek J, 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. PMID: 22228807.

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