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Tofacitinib Prodrug-1

CAS No. :

MCE 国际站：Tofacitinib Prodrug-1

产品活性：Tofacitinib Prodrug-1 是减轻托法替尼 (Tofacitinib) 全身性不良反应的口服有效前药。Tofacitinib Prodrug-1 能在小鼠模型有效减轻恶唑酮诱导的结肠炎，具有低毒性，是治疗溃疡性结肠炎的潜在候选药物。

研究领域：Epigenetics | Stem Cell/Wnt | JAK/STAT Signaling | Apoptosis

作用靶点：JAK | Apoptosis

In Vitro: Tofacitinib Prodrug-1 (compound 20g) (1 mM; 12 hours at 37 °C) is not obviously degraded from 0 to 12 hours in simulated gastric ａnd intestinal fluid.

In Vivo: Tofacitinib Prodrug-1 (22.5 mg/kg; p.o.) can decrease the systemic exposure of tofacitinib by releasing the parent drug Tofacitinib into the circulation slowly.
Tofacitinib Prodrug-1 (22.5 mg/kg; p.o.) can increase intestinal exposure to improve the therapeutic effect of Tofacitinib.
Tofacitinib Prodrug-1 (1.5 mg/kg; p.o.; twice daily, for 4 days) can effectively attenuate the oxazolone-induced colitis in mice.
Tofacitinib Prodrug-1 (1.5 mg/kg; i.g.; twice daily, for 4 days) has no apparent influence on systemic immunosuppression in normal mice, which could decrease the risk of infection associated with Tofacitinib.
Tofacitinib Prodrug-1 (2000 mg/kg; i.g.; single) has low toxicity ａnd was tolerated at an oral dose of 2000 mg/kg, ａnd no significant change was observed in biochemical parameters ａnd organ indexes.

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