An inhibitor of TG2
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ZED-1227

Item No. 42333

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(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-heptenoic acid, methyl ester
CAS Number
1542132-88-6
Synonyms
  • TAK-227
Molecular Formula
C26H36N6O6
Formula Weight
528.6
Purity
≥95%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Slightly soluble: 0.1-1 mg/ml
SMILES
O=C([C@@H](NC(C1=CN=CN1C)=O)CC/C=C/C(OC)=O)NC2=CC=CN(CC(NCC(CC)CC)=O)C2=O
InChi Code
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
InChi Key
VHGWUSABWIEXKQ-BEBFYNPSSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $99

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    5 mg

    $371

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    10 mg

    $545

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    25 mg

    $743

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    Product Description

    ZED-1227 is an inhibitor of transglutaminase 2 (TG2; IC50 = 0.053 µM).1 It is selective for TG2 over TG1, TG3, TG6, and Factor XIIIa2 (IC50s = 24.86, >50, 6.44, and >50 µM, respectively). ZED-1227 (25 and 50 mg/kg) increases the duodenal villous height-to-crypt depth ratio and reduces the percentage of CD3+ duodenal intraepithelial lymphocytes and CD138+ duodenal plasma cells in a humanized mouse model of celiac disease.2 It also increases duodenal expression of Tgfb1, Aldh1a2, and other genes associated with regulatory immune responses and epithelial adaptation in the same model.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Büchold, C., Hils, M., Gerlach, U., et al. Features of ZED1227: The first-in-class tissue transglutaminase inhibitor undergoing clinical evaluation for the treatment of celiac disease. Cells 11(10), 1667 (2022).

    2. Pesi, A., Encalada-Ventura, M.A., Mard, H.E.L., et al. A humanized celiac disease mouse model reflects histologic and immune effects of transglutaminase inhibition in patients. Gastroenterolgy (2026).