Baricitinib phosphate
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.
已表明，JAKs的直接和间接抑制快速且持久地改善临床疾病的治疗方案。Baricitinib phosphate（INCB 028050）是一种选择性JAK1和JAK2抑制剂。
体外实验：Baricitinib phosphate是一种有效的选择性JAK1/JAK2口服抑制剂，对JAK1和JAK2的纳摩尔效力分别为5.9 nM和5.7 nM，约是JAK3和Tyk2的10倍，对c-Met和Chk2无抑制活性。INCB028050在浓度为50 nM时，抑制包括IL-6和IL-23在内的多种促炎细胞因子的信号传导[1]。
体内实验：在大鼠佐剂性关节炎模型中，baricitinib phosphate显示出显著的疗效。一定剂量的baricitinib phosphate部分和/或周期性地抑制JAK1/JAK2的活性，对JAK3无抑制作用。Baricitinib phosphate在多种关节炎小鼠模型中也有效，没有证据表明baricitinib phosphate有抑制体液免疫或不良血液效应等副反应[2]。
临床试验：在健康人和类风湿性关节炎患者中进行了一些临床试验，已经进行了PK、有效性和DDI的研究。
参考文献：
[1] Fridman JS, Scherle PA, Collins R, Burn TC, Li Y, Li J, Covington MB, Thomas B, Collier P, Favata MF, Wen X, Shi J, McGee R, Haley PJ, Shepard S, Rodgers JD, Yeleswaram S, Hollis G, Newton RC, Metcalf B, Friedman SM, Vaddi K. Selective inhibition of JAK1 and JAK2 is efficacious in rodent models of arthritis: preclinical characterization of INCB028050. J Immunol. 2010;184(9):5298-307.
| Storage | Store at -20°C |
| M.Wt | 469.41 |
| Cas No. | 1187595-84-1 |
| Formula | C16H20N7O6PS |
| Synonyms | INCB 028050;LY 3009104;INCB028050;LY3009104;LY-3009104;INCB-028050 |
| Solubility | insoluble in EtOH; insoluble in H2O; ≥172.6 mg/mL in DMSO |
| Chemical Name | 2-[1-ethylsulfonyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)pyrazol-1-yl]azetidin-3-yl]acetonitrile;phosphoric acid |
| SDF | Download SDF |
| Canonical SMILES | CCS(=O)(=O)N1CC(C1)(CC#N)N2C=C(C=N2)C3=C4C=CNC4=NC=N3.OP(=O)(O)O |
| 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。 |
质量控制和MSDS
- 批次:
化学结构
