Cat. No. Name Size Price Add Cart
KI2505RN4861 mg$910
RN4865 mg$2470
RN48610 mg$3770

Chemical Characteristic

Product NameRN486
SynonymsN/A
CAS No.1242156-23-5
Molecular Weight 606.69
FormulaC35H35FN6O3
Chemical Name6-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
Smilesc1(=O)n(ccc2cc(cc(c12)F)C1CC1)c1c(c(ccc1)c1cn(c(=O)c(c1)Nc1ccc(cn1)N1CCN(CC1)C)C)CO
Chemical Structure

Biological activities

RN486 is a potent, selectively and proprietary Bruton's tyrosine kinase (Btk) inhibitor. RN486 inhibits Btk activity with an IC50 of 4.0 nM. RN486 blocks Fce receptor cross-linking- induced degranulation in mast cells with an IC50 of 2.9 nM, and inhibits Fcg receptor engagement-mediated tumor necrosis factor a production in monocytes with an IC50 of 7.0 nM. RN486 also inhibits B cell antigen receptor-induced expression of CD69 in B cells in whole blood with an IC50 of 21.0 nM. In vivo in adjuvant-induced arthritis (AIA) models in rat, RN486 inhibits both joint and systemic inflammation, reducing both paw swelling and inflammatory markers in the blood.[1]

Protocols

In vivo, RN486 is dissolved in DMSO.[1]

References

[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, 341(1): 90-103.

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