Description
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.
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