| 產(chǎn)品描述： | RN486 is a potent, selective and orally active Btk inhibitor with an IC50 of 4.0 nM and a Kd of 0.31 nM. RN486 is less active for other kinases. RN486 can be used for rheumatoid arthritis and systemic lupus erythematosus research |
| 靶點： |
IC50: 4.0 nM (Btk) Kd: 0.31 nM (Btk);BTK |
| 體外研究： |
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). 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 |
| 體內(nèi)研究： |
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 |
| 參考文獻： |
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. |
| 溶解性： |
soluble in DMSO |
| 保存條件： |
-20℃ |
| 配置溶液濃度參考： |
|
1mg |
5mg |
10mg |
| 1 mM |
1.648 ml |
8.241 ml |
16.483 ml |
| 5 mM |
0.33 ml |
1.648 ml |
3.297 ml |
| 10 mM |
0.165 ml |
0.824 ml |
1.648 ml |
| 50 mM |
0.033 ml |
0.165 ml |
0.33 ml |
|
| 注意： |
部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。 |
上海工商
危險品化學(xué)品經(jīng)營許可證（不帶存儲）
營業(yè)執(zhí)照(三證合一)
北京