[CAS NO. 1242156-23-5] RN486
PRODUCTS SPECIFICATIONS [1242156-23-5]
DESCRIPTION [1242156-23-5]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 606.69 |
| Molecular Formula | C35H35FN6O3 |
| SMILES | 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 |
3 Publications Citing Use of MCE
Summary
In Vitro
RN486 blocks 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 nM), and B cell antigen receptor-induced expression of an activation marker, CD69, in B cells in whole blood (IC
50
= 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]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
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] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 24 mg/mL ( 39.56 mM ; Need ultrasonic and warming)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.6483 mL | 8.2414 mL | 16.4829 mL |
| 5 mM | 0.3297 mL | 1.6483 mL | 3.2966 mL |
| 10 mM | 0.1648 mL | 0.8241 mL | 1.6483 mL |
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 Apr;341(1):90-103.
- [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.
- [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.