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

ZED-1227 

Cat. No.: HY-19359 Purity: 99.97%
Handling Instructions

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).

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

ZED-1227 Chemical Structure

ZED-1227 Chemical Structure

CAS No. : 1542132-88-6

Size Price Stock Quantity
1 mg USD 350 In-stock
Estimated Time of Arrival: December 31
5 mg USD 780 In-stock
Estimated Time of Arrival: December 31
10 mg USD 1250 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 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)[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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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 the small intestinal mucosa[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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
Solvent & Solubility
In Vitro: 

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

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8918 mL 9.4589 mL 18.9179 mL
5 mM 0.3784 mL 1.8918 mL 3.7836 mL
10 mM 0.1892 mL 0.9459 mL 1.8918 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: 2.08 mg/mL (3.93 mM); Suspended solution; Need ultrasonic

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (3.93 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (3.93 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 99.97%

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Keywords:

ZED-1227ZED1227ZED 1227GlutaminaseInhibitorinhibitorinhibit

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Product Name:
ZED-1227
Cat. No.:
HY-19359
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