TY-51469是糜蛋白酶(chymase)抑制剂，在类人猿和人糜蛋白酶的IC50值分别为0.4和7.0nM。
TY-51469 is a chymase inhibitor with IC50s for simian and human chymases of 0.4 and 7.0 nM, respectively.
TY-51469 shows 100% stability in rat plasma at 40°C for as long as 1 hour[1]. TY-51469 suppresses the accumulation of neutrophils in the lung and reduces silica-induced pulmonary fibrosis in mice[2].
[1]. Takato H, et al. The specific chymase inhibitor TY-51469 suppresses the accumulation of neutrophils in the lung and reduces silica-induced pulmonary fibrosis in mice. Expert Opinion on Therapeutic Targets Volume 15, 2011 - Issue 4.
Animal experiment: | Rats[1] The 2-week intravenous repeated-dose toxicity study of TY-51469 was conducted in male Sprague-Dawley rats at daily doses of 0 (control), 20, and 60 mg/kg[1].Mice[1]the chymase inhibitor TY-51469 was administered daily at a dose of 0.1 or 1.0 mg/kg/day for 21 days using an osmotic pump to male 8-week-old ICR mice. The osmotic pump released the drug solution continuously at a rate of 0.3 μL/h for 21 days[2]. |
参考文献: [1]. Takato H, et al. The specific chymase inhibitor TY-51469 suppresses the accumulation of neutrophils in the lung and reduces silica-induced pulmonary fibrosis in mice. Expert Opinion on Therapeutic Targets Volume 15, 2011 - Issue 4. | |
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