ZED-1227 is a specific and orally active transglutaminase 2 (TG2) inhibitor, with an IC 50 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) In Vitro 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: BALB/c miceDosage: 5 mg/kg Administration: Oral gavage Result: Inhibited TG2 in vivo in the small intestinal mucosa. Form:Solid IC50& Target:IC50: 45 nM (TG2)
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ZED-1227
CAS number：1542132-88-6 molecular formula：C26H36N6O6
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| Chinese alias | - | ||
| English alias | GTPL12802 | methyl (E,6S)-7-[[1-[2-(2-ethylbutylamino)-2-oxoethyl]-2-oxopyridin-3-yl]amino]-6-[(3-methylimidazole-4-carbonyl)amino]-7-oxohept-2-enoate | GLUTAMINASE | Methyl (2E,6S)-7-((1-(2-((2-ethylbutyl)amino)-2-oxoethyl)-1,2-dihydro-2-oxo-3-pyridinyl) | ||
| CAS number | 1542132-88-6 | molecular formula | C26H36N6O6 |
| molecular weight | 528.6 g/mol | Exact mass | ≥98.0% |
| PSA | 152.000 Ų | logp | 1.600 |
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