Tofacitinib citrate

Product introduction:

Tofatinib citrate is an oral JAKs inhibitor. The half effective concentrations (IC50) of Jak1, JAK2 and JAK3 in vitro are 3.2, 4.1 and 1.6 nmol / L respectively. In cell experiment, the ability of selective inhibition of JAK3 is more than 10 times higher than that of JAK2. Tofatinib citrate can interact with the receptors of cytokines IL-2, 4, 7 and 9 necessary to activate T cells γ Common chain combination. This drug is effective in the mouse model of heart transplantation, which shows that T cells play a vital role in transplantation rejection. In addition, tofatinib citrate can inhibit TNF and IFN by acting on human monocytes and synovial cells- γ、 Reduce IL-6, chemokine production and T cell CD4 proliferation. Animal experiments showed that the drug could significantly reduce joint swelling in adjuvant induced arthritis rat model and collagen induced arthritis mouse model, and significantly improve synovitis and cartilage damage compared with the control group.

CAS：540737-29-9

Molecular formula: C₁₆H₂₀N₆O.C₆H₈O₇

Molecular weight: 504.497

Structural type:

Product purpose: Tofacitinib citrate combined with methotrexate in the treatment of active rheumatoid arthritis with insufficient response to tumor necrosis factor inhibitors.