Tofacitinib - 13 C 3, 15 N (Tasocitinib- 13 C 3, 15 N; CP-690550- 13 C 3, 15 N) is the 15 N, 13 C-labeled Tofacitinib. Tofacitinib (Tasocitinib) is an orally active, blood-brain barrier permeable selective inhibitor of JAK1 / JAK3. Tofacitinib blocks the JAK-STAT/NF-κB signaling pathway, inhibits cytokine signal transduction, phosphorylation of STAT1/STAT5, and suppresses innate and adaptive immune responses. Tofacitinib can be used in research related to major depressive disorder, rheumatoid arthritis, pulmonary diseases, systemic lupus erythematosus, and immune-mediated liver injury [1] [2] [3] [4] [5] [6] [7] [8] [9].
References:
[1]. Gao YN, et al. Tofacitinib prevents depressive-like behaviors through decreased hippocampal microgliosis and increased BDNF levels in both LPS-induced and CSDS-induced mice. Acta pharmacologica Sinica. 2025 Feb;46(2):353-365.
[2]. Sendo S, et al. Tofacitinib facilitates the expansion of myeloid-derived suppressor cells and ameliorates interstitial lung disease in SKG mice. Arthritis research & therapy. 2019 Aug 06;21(1):184.
[3]. Zhang X, et al. Tofacitinib reduces acute lung injury and improves survival in a rat model of sepsis by inhibiting the JAK-STAT/NF-κB pathway. Journal of inflammation (London, England). 2023 Feb 03;20(1):5.
[4]. Wang W, et al. The JAK/STAT pathway is activated in systemic sclerosis and is effectively targeted by tofacitinib. Journal of scleroderma and related disorders. 2020 Feb;5(1):40-50.
[5]. Wei X, et al. Development of a Janus Kinase Inhibitor Prodrug for the Treatment of Rheumatoid Arthritis. Molecular pharmaceutics. 2018 Aug 06;15(8):3456-3467.
[6]. Fleischmann R, et al. Placebo-controlled trial of tofacitinib monotherapy in rheumatoid arthritis. N Engl J Med. 2012 Aug 9;367(6):495-507.
[7]. Sandborn WJ, et al. Tofacitinib, an oral Janus kinase inhibitor, in active ulcerative colitis. N Engl J Med. 2012 Aug 16;367(7):616-24.
[8]. Furumoto Y, et al. Tofacitinib Ameliorates Murine Lupus and Its Associated Vascular Dysfunction. Arthritis & rheumatology (Hoboken, N.J.). 2017 Jan;69(1):148-160.
[9]. Wang H, et al. The JAK inhibitor tofacitinib ameliorates immune‑mediated liver injury in mice. Molecular medicine reports. 2019 Dec;20(6):4883-4892.
References:
[1]. Gao YN, et al. Tofacitinib prevents depressive-like behaviors through decreased hippocampal microgliosis and increased BDNF levels in both LPS-induced and CSDS-induced mice. Acta pharmacologica Sinica. 2025 Feb;46(2):353-365.
[2]. Sendo S, et al. Tofacitinib facilitates the expansion of myeloid-derived suppressor cells and ameliorates interstitial lung disease in SKG mice. Arthritis research & therapy. 2019 Aug 06;21(1):184.
[3]. Zhang X, et al. Tofacitinib reduces acute lung injury and improves survival in a rat model of sepsis by inhibiting the JAK-STAT/NF-κB pathway. Journal of inflammation (London, England). 2023 Feb 03;20(1):5.
[4]. Wang W, et al. The JAK/STAT pathway is activated in systemic sclerosis and is effectively targeted by tofacitinib. Journal of scleroderma and related disorders. 2020 Feb;5(1):40-50.
[5]. Wei X, et al. Development of a Janus Kinase Inhibitor Prodrug for the Treatment of Rheumatoid Arthritis. Molecular pharmaceutics. 2018 Aug 06;15(8):3456-3467.
[6]. Fleischmann R, et al. Placebo-controlled trial of tofacitinib monotherapy in rheumatoid arthritis. N Engl J Med. 2012 Aug 9;367(6):495-507.
[7]. Sandborn WJ, et al. Tofacitinib, an oral Janus kinase inhibitor, in active ulcerative colitis. N Engl J Med. 2012 Aug 16;367(7):616-24.
[8]. Furumoto Y, et al. Tofacitinib Ameliorates Murine Lupus and Its Associated Vascular Dysfunction. Arthritis & rheumatology (Hoboken, N.J.). 2017 Jan;69(1):148-160.
[9]. Wang H, et al. The JAK inhibitor tofacitinib ameliorates immune‑mediated liver injury in mice. Molecular medicine reports. 2019 Dec;20(6):4883-4892.