Baricitinib phosphate

产品说明书

Print
Chemical Structure| 1187595-84-1 同义名 : 磷酸巴瑞西替尼 ;INCB028050 phosphate; LY3009104 phosphate
CAS号 : 1187595-84-1
货号 : A214136
分子式 : C16H20N7O6PS
纯度 : 98%
分子量 : 469.41
MDL号 : MFCD25976707
存储条件:

Pure form Sealed in dry,2-8°C

In solvent -20°C:3-6个月-80°C:12个月

溶解度 : -
动物实验配方:
生物活性
描述 Baricitinib (INCB028050) is demonstrated as a potent inhibitor of Janus kinase (JAK) signaling and functionality in cell-based assays. In peripheral blood mononuclear cells (PBMCs), Baricitinib curtails IL-6-induced phosphorylation of STAT3 (pSTAT3) and the subsequent secretion of the chemokine MCP-1, with IC50 values being 44 nM and 40 nM, respectively. Furthermore, in isolated naive T-cells, it suppresses pSTAT3 activation by IL-23 with an IC50 value of 20 nM, significantly inhibiting the production of IL-17 and IL-22, two cytokines produced by Th17 cells, known for their inflammatory and pathogenic roles, with an IC50 of 50 nM. This is in sharp contrast to structurally similar but less effective JAK1/2 inhibitors INCB027753 and INCB029843, which show no notable effect in these assay systems up to 10 μM[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.13mL

0.43mL

0.21mL

10.65mL

2.13mL

1.07mL

21.30mL

4.26mL

2.13mL

参考文献

[1]Fridman JS, et al. Selective inhibition of JAK1 and JAK2 is efficacious in rodent models of arthritis: preclinical characterization of INCB028050. J Immunol. 2010 May 1;184(9):5298-307.

[2]Jabbari A, et al. Reversal of Alopecia Areata Following Treatment With the JAK1/2 Inhibitor Baricitinib. EBioMedicine. 2015 Feb 26;2(4):351-5.