ZED-1227

• CAT Number: I010144
• CAS Number: 1542132-88-6
• Molecular Formula: C26H36N6O6
• Molecular Weight: 528.60
• Purity: ≥95%
• Synonyms: 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
• InChI: InChI=1S/C26H36N6O6/c1-5-18(6-2)14-28-22(33)16-32-13-9-11-20(26(32)37)30-24(35)19(10-7-8-12-23(34)38-4)29-25(36)21-15-27-17-31(21)3/h8-9,11-13,15,17-19H,5-7,10,14,16H2,1-4H3,(H,28,33)(H,29,36)(H,30,35)/b12-8+/t19-/m0/s1
• InChIKey: VHGWUSABWIEXKQ-BEBFYNPSSA-N
• SMILES: CCC(CC)CNC(=O)CN1C=CC=C(C1=O)NC(=O)C(CCC=CC(=O)OC)NC(=O)C2=CN=CN2C

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].
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].
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].

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.