ZED-1227 is a specific and orally active transglutaminase 2 (TG2) inhibitor, with an IC50 of 45 nM. ZED-1227 can block inflammation-induced TG2 expression and activity. ZED-1227 can be used for the research of celiac disease (CeD).
IC50&Target
IC50: 45 nM (TG2)
体外研究
ZED-1227 (0.1 μΜ-1 μΜ; 24 hours) has no effect on metabolic activity and proliferation in Huh7 cells and CaCo2 cells, that suggests ZED-1227 has no cytotoxic activity.
ZED-1227 (0.002-0.2 mg/mL; 30 minutes) inhibits TG2 in the small intestinal mucosa in vitro.
体内研究
ZED-1227 reduces the activity of intestinal TG2 induced by Polyinosinic:Polycytidylic acid (40 mg/kg) to normal control levels and subdues intestinal inflammation in mice.
ZED-1227 (5 mg/kg; i.g.) is able to inhibit TG2 in the small intestinal mucosa.
Animal Model:
BALB/c mice
Dosage:
5 mg/kg
Administration:
Oral gavage
Result:
Inhibited TG2 in vivo in the small intestinal mucosa.
分子式
C26H36N6O6
分子量
528.60
CAS号
1542132-88-6
运输条件
Room temperature in continental US; may vary elsewhere.