1. Metabolic Enzyme/Protease
  2. Glutaminase
  3. ZED-1227

ZED-1227 

Cat. No.: HY-19359 Purity: 99.32%
Handling Instructions

ZED-1227 is a specific and oral transglutaminase 2 (TG2) inhibitor, with an IC50 of 45 nM. ZED-1227 can block inflammation-induced TG2 expression and activity. ZED-1227 is a promising agent for the treatment of celiac disease (CeD).

For research use only. We do not sell to patients.

ZED-1227 Chemical Structure

ZED-1227 Chemical Structure

CAS No. : 1542132-88-6

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1 mg USD 350 In-stock
Estimated Time of Arrival: December 31
5 mg USD 780 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

ZED-1227 is a specific and oral transglutaminase 2 (TG2) inhibitor, with an IC50 of 45 nM. ZED-1227 can block inflammation-induced TG2 expression and activity. ZED-1227 is a promising agent for the treatment of celiac disease (CeD)[1][2].

IC50 & Target

IC50: 45 nM (TG2)[2]

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[2].
ZED-1227 (0.002-0.2 mg/mL; 30 minutes) inhibits TG2 in the small intestinal mucosa in vitro[2].

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[1].
ZED-1227 (5 mg/kg; i.g.) is able to inhibit TG2 in vivo in the small intestinal mucosa[2].

Animal Model: BALB/c mice[2]
Dosage: 5 mg/kg
Administration: Oral gavage
Result: Inhibited TG2 in vivo in the small intestinal mucosa.
Molecular Weight

528.60

Formula

C₂₆H₃₆N₆O₆

CAS No.

1542132-88-6

SMILES

O=C(OC)/C=C/CC[[email protected]](NC(C1=CN=CN1C)=O)C(NC2=CC=CN(CC(NCC(CC)CC)=O)C2=O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
References
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Keywords:

ZED-1227ZED1227ZED 1227GlutaminaseInhibitorinhibitorinhibit

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ZED-1227
Cat. No.:
HY-19359
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