| Bioactivity | 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)[1][2]. | ||||||||||||
| Target | IC50: 45 nM (TG2) | ||||||||||||
| Invitro | 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[2].ZED-1227 (0.002-0.2 mg/mL; 30 minutes) inhibits TG2 in the small intestinal mucosa in vitro[2]. | ||||||||||||
| 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[1].ZED-1227 (5 mg/kg; i.g.) is able to inhibit TG2 in the small intestinal mucosa[2]. Animal Model: | ||||||||||||
| Name | ZED-1227 | ||||||||||||
| CAS | 1542132-88-6 | ||||||||||||
| Formula | C26H36N6O6 | ||||||||||||
| Molar Mass | 528.60 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Manu Encalada, et al. The Oral Transglutaminase 2 (TG2) Inhibitor Zed1227 Blocks TG2 Activity in a Mouse Model of Intestinal Inflammation. Gastroenterology. 154(6):S-490. [2]. Christian Büchold, et al. Pyridinone derivatives as tissue transglutaminase inhibitors. WO2014012858A1. |
ZED-1227
CAS: 1542132-88-6 F: C26H36N6O6 W: 528.60
ZED-1227 is a specific and orally active transglutaminase 2 (TG2) inhibitor,with an IC50 of 45 nM. ZED-1227 can block in
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