| Catalog Number： |
R30000 |
|
CAS No.: |
1242156-23-5 |
| MDL: |
|
|
Formula: |
C35H35FN6O3 |
| F.W.: |
606.69 |
|
Purity: |
99％ |
| Package: |
|
|
Unit: |
mg |
| Appearance: |
|
|
M.P.: |
|
| B.P.: |
|
|
Density: |
|
| Optical Rotation: |
|
|
Refractive Index: |
|
| Solubility: |
Soluble in DMSO |
|
Stability: |
|
| Storage: |
Store at 0°C (short term), -20°C (long term) |
|
Category: |
Reference Standard |
| Reference: |
Xu, D. et al.: J. Pharmacol. Exp. Ther., 34, 90 (2012); P. Mina-Osorio, et al, Suppression of glomerulonephritis in lupus-prone NZB × NZW mice by RN486, a selective inhibitor of Brutons tyrosine kinase, Arthritis Rheum. 2013 Sep;65(9):2380-91. doi: 10.1002/art.38047. |
| Application: |
RN 486 is a Bruton’s tyrosine kinase (Btk) inhibitor, blocking receptor cross-linking-induced degranulation in mast cells. May be used in the prevention of arthritis and other autoimmune diseases.RN486 is a selective, and reversible inhibitor of Brutons tyrosine kinase (BTK), binding to the enzyme potently and competitively with an in vitro IC50 of 4.0 nM (enzymatic assay), and 0.3 nM (FRET binding assay). Highly selective over almost all other kinases including Syk and JAK, two validated RA (Rheumatoid Arthritis) targets. It exhibits an excellent pharmacokinetic profile, and displayed strong functional as well as disease-related activities by inhibiting immune responses mediated by two important immunoreceptors, BCR and FcR, in both human cells and rodents, producing dose dependent efficacy in both CIA and AIA, with evidence for substantial efficacy in combination with low-dose methotrexate. |
| Category: |
|
