Pharmaceutical raw materials powder Baricitinib

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Baricitinib powder Usage and Synthesis.

Baricitinib (olumiant) is a selective JAK2 and JAK1 inhibitor with little efficacy against JanusKinase, jak3orTYK2. This kinase and its associated signal transduction and transcriptional activator (JAK-STAT) are major intracellular pathways that control the magnitude and duration of cytokine signaling with type I and type II cytokine receptors. These receptors lack the ability to mediate intrinsic enzyme activity signal transduction; The Janus kinase \ signaling and transcriptional activator is phosphorylated by the JAK enzyme, leading to STAT activation. Several inflammatory factors are involved in the pathogenesis of RA, including IL-6, granulocyte macrophage colony-stimulating factor, and GM-CSF factor. Interferon signals are transmitted through the JAK-STAT signaling pathway. Thus, JAK1 and JAK2 inhibitors can target multiple RA-related cytokine pathways, thereby reducing the activation and proliferation of immune cells key to inflammatory cells. Baricitinib has no effect on JAK3. JAK3 may be related to common gamma chain receptors. Common gamma-chain cytokines include IL-15 and IL-21, which play a major role in lymphocyte activation, function and proliferation.

Uses of Baricitinib powder.

1. For adults with moderate to severe active rheumatoid arthritis (RA), patients who are intolerant to one or more antirheumatic drugs can be treated with this product as a single drug or in combination with methotrexate. The efficacy of baricitinib in the treatment of psoriasis, diabetic nephropathy, atopic dermatitis, systemic lupus erythematosus and other diseases is currently in the phase II clinical stage.

2. Used in scientific research and chemical reagent field.

In vitro study of Baricitinib.

In peripheral blood mononuclear cells, Baricitinib inhibited the phosphorylation of STAT3(pSTAT3), a typical substrate stimulated by IL-6, and the subsequent production of chemokine MCP-1, with IC50 values of 44nM and 40nM, respectively. Baricitinib also inhibited IL-23-stimulated STAT3 phosphorylation in independent naive T cells with an IC50 of 20nM.

Product method of Bulk Baricitinib powder.

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