生物活性 | |||
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描述 | BB-Cl-amidine is a novel pan-PAD inhibitor with potency to PAD1-4, with half-life of 1.75h in vivo. BB-Cl-amidine exhibited potency against U2OS osteosarcoma cell viability with EC50 value of 8.8μM post 72-hour treatment. Inhibition of PAD by 20μM or 200μM BB-Cl-amidine could prevent PMA-induced neutrophil extracellular trap formation of bone marrow neutrophils prepared from 8-week-old MRL/lpr mice. And this effect could be observed in an in vivo study of MRL/lpr mice daily subcutaneous injected with BB-Cl-amidine at dose of 1mg/kg from 8 to 14 weeks of age. And improved vascular function, and decreasesd IFN signature in bone marrow and kidney, decreased IC deposition in kidneys and reduced proteinuria, improved skin involvement could be found after administration of BB-Cl-amidine. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.17mL 0.43mL 0.22mL |
10.87mL 2.17mL 1.09mL |
21.74mL 4.35mL 2.17mL |