Baricitinib (olumiant) has the cas number of 1187594-09-7 is a selective JAK2 and JAK1 inhibitor that targets multiple active rheumatoid arthritis-associated cytokine pathways, thereby reducing the activation and proliferation of key immune cells in inflammatory cells. It is mainly used to treat moderate to severe active rheumatoid arthritis in adults. Patients can be treated with Baricitinib for one or more anti-rheumatic drug intolerance. It can be treated with monotherapy or with methotrexate. Baricitinib is currently in Phase II clinical stage in the treatment of psoriasis, diabetic nephropathy, atopic dermatitis, systemic lupus erythematosus and other diseases.
In vitro studies have shown that Baricitinib cas number 1187594-09-7 inhibits IL-6-stimulated phosphorylation of the typical substrate STAT3 (pSTAT3) and subsequent production of the chemokine MCP-1 in peripheral blood mononuclear cells with IC50 values of 44 nM and 40 nM, respectively. Baricitinib also inhibits IL-23-stimulated phosphorylation of STAT3 in independent naive T cells with an IC50 of 20 nM.
In vivo studies have shown that Baricitinib inhibits IL-6-stimulated STAT3 phosphorylation in whole blood with an IC50 of 128 nM. Baricitinib is expected to inhibit JAK1/2 signaling in rats for 8 hours. It can also inhibit disease in a rat model of adjuvant arthritis but has dose-dependent properties. The use of Baricitinib for 2 consecutive weeks per day provides an imaging improvement in the normal structure and appearance of the ankle and tibia of the rat model of adjuvant arthritis. Baricitinib (10 mg/mL, orally) increased the joint damage score of the mouse collagen-induced arthritis (CIA) model by 47%. In the collagen antibody-induced arthritis (CAIA) mouse model, It can reduce 74% of vasospasm and 78% of bone damage, improve cartilage damage and inflammatory signals, and increase the disease composite score by 53%. Baricitinib is effective in patients with active rheumatoid arthritis, and most of the disease modifying drugs and biological agents are difficult to be effective. Baricitinib preferentially inhibits JAK1 and JAK2, with selectivity 10 times higher than Tyk2 and 100 times higher than JAK3. The use of Baricitinib has a strict dose limit, otherwise it will induce anemia, which is caused by the effect on JAK2, but its efficacy is very clear anyway.
Thera Category: JAK Inhibitor
Cas No.: 1187594-09-7
Synonym: 1-(Ethylsulfonyl)-3-[4-(7H-pyrrolo[2,3-d]pyriMidin-4-yl)-1H-pyrazol-1-yl]-3-azetidineacetonitrile;Baricitinib;INCB 028050;LY 3009104;Baricitinib (LY3009104);Baricitinib/INCB 028050/LY3009104;Baricitinib (LY3009104, INCB028050);2-(3-(4-(3H-Pyrrolo[2,3-d]pyriMidin-4-yl)-1H-pyrazol-1-yl)-1-(ethylsulfonyl)azetidin-3-yl)acetonitrile
Molecular Formula: C16H17N7O2S
Molecular Weight: 371.41688
Specifications: Available on request
Packing:Export worthy packing
Material Safety Data Sheet:Available on request
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