RO9021
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
IC50为5.6 nM。
RO9021是一种Syk抑制剂。
脾酪氨酸激酶(SYK)是由激活的免疫受体(如Fc受体和B细胞受体(BCR))调节的细胞内信号的关键集成器,对于淋巴样细胞的功能和发育具有极大重要性。
体外:先前研究发现,除了抑制人外周血单核细胞和全血中的B细胞受体信号传导、人单核细胞中的FcγR信号传导和人肥大细胞中的FcR信号传导外,RO9021还可以阻断小鼠骨髓巨噬细胞的体外破骨细胞形成。此外,RO9021可以阻断人B细胞中的Toll样受体9信号传导,导致B细胞分化时成纤维细胞、免疫球蛋白(Ig)G和IgM的水平降低。另外,RO9021还可以通过TLR9激活,有效抑制人类浆细胞样树突状细胞(pDC)产生I型干扰素,并且研究发现这种效应对TLR9是特异性的,因为RO9021对TLR4或JAK-STAT介导信号传导未显示出抑制作用[1]。
体内:动物研究表明,口服给药RO9021可显著抑制mCIA模型中的关节炎进展,观察到药代动力学-药效学相关性[1]。
临床试验:到目前为止,RO9021仍处于临床前研究阶段。
参考文献:
[1] Liao C, et al. Selective inhibition of spleen tyrosine kinase (SYK) with a novel orally bioavailable small molecule inhibitor, RO9021, impinges on various innate and adaptive immune responses: implications for SYK inhibitors in autoimmune disease therapy. Arthritis Res Ther. 2013 Oct 4;15(5):R146.
Storage | Store at -20°C |
M.Wt | 355.44 |
Cas No. | 1446790-62-0 |
Formula | C18H25N7O |
Solubility | Soluble in DMSO |
Chemical Name | 6-(((1R,2S)-2-aminocyclohexyl)amino)-4-((5,6-dimethylpyridin-2-yl)amino)pyridazine-3-carboxamide |
SDF | Download SDF |
Canonical SMILES | O=C(C1=NN=C(N[C@H]2[C@@H](N)CCCC2)C=C1NC3=NC(C)=C(C)C=C3)N |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |