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ZED1227

Chemical Structure : ZED1227

CAS No.: 1542132-88-6

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ZED1227 (ZED-1227)

Catalog No.: PC-38770Not For Human Use, Lab Use Only.

ZED1227 is a potent, selective, covalent, and orally active transglutaminase 2 (TGase 2, TG2) inhibitor with IC50 of 45 nM.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

ZED1227 is a potent, selective, covalent, and orally active transglutaminase 2 (TGase 2, TG2) inhibitor with IC50 of 45 nM.
ZED1227 selectively binds to the active state of TG2, forming a stable covalent bond with the cysteine in TG2 catalytic center.
ZED1227 blocks inflammation-induced TG2 expression and activity, inhibits TG2 in the small intestinal mucosa in vitro, with no sginificant cytotoxic activity.
ZED1227 reduces the activity of intestinal TG2 induced by polyinosinic:polycytidylic acid (40 mg/kg) to normal control levels and subdues intestinal inflammation in mice.
ZED1227 shows potential for treatment and research of celiac disease.

Physicochemical Properties

M.Wt 528.610
Formula C26H36N6O6
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

Methyl (2E,6S)-7-[[1-[2-[(2-ethylbutyl)amino]-2-oxoethyl]-1,2-dihydro-2-oxo-3-pyridinyl]amino]-6-[[(1-methyl-1H-imidazol-5-yl)carbonyl]amino]-7-oxo-2-heptenoate

References

1. Büchold C, et al. Cells. 2022 May 17;11(10):1667.

2. Schuppan D, et al. N Engl J Med. 2021 Jul 1;385(1):35-45.

3. Manu Encalada, et al. Gastroenterology. 154(6):S-490.

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