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).

Product information

CAS Number: 1542132-88-6

Molecular Weight: 528.60

Formula: C26H36N6O6

Chemical Name: methyl (2E,6S)-6-[(1-{[(2-ethylbutyl)carbamoyl]methyl}-2-oxo-1,2-dihydropyridin-3-yl)carbamoyl]-6-[(1-methyl-1H-imidazol-5-yl)formamido]hex-2-enoate

Smiles: CN1C=NC=C1C(=O)N[C@@H](CC/C=C/C(=O)OC)C(=O)NC1=CC=CN(CC(=O)NCC(CC)CC)C1=O

InChiKey: VHGWUSABWIEXKQ-BEBFYNPSSA-N

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

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 125 mg/mL (236.47 mM; Need ultrasonic).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

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. ZED-1227 (0.002-0.2 mg/mL; 30 minutes) inhibits TG2 in the small intestinal mucosa in vitro.

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. ZED-1227 (5 mg/kg; i.g.) is able to inhibit TG2 in the small intestinal mucosa.

Products are for research use only. Not for human use.