ZED1227 | TG2 inhibitor | Probechem Biochemicals

Chemical Structure : ZED1227

CAS No.: 1542132-88-6

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ZED1227 (ZED-1227)

货号: 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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5 mg	￥3580	In stock
10 mg	￥5480	In stock
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100 mg		Get quote

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生物&药学活性

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.

物理化学性质&存储条件

分子量	528.610
分子式	C26H36N6O6
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
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

参考文献

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.

ZED1227 (ZED-1227)

生物&药学活性

物理化学性质&存储条件

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ZED1227 (ZED-1227)

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