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ZED-1227 (TAK-227) is an orally active, selective and potent transglutaminase 2 (TG2) inhibitor with anticancer activity that blocks inflammation-induced TG2 expression and activation for the treatment of Celiac Disease.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $261 | In Stock | In Stock | |
| 2 mg | $368 | In Stock | In Stock | |
| 5 mg | $535 | In Stock | In Stock | |
| 10 mg | $817 | In Stock | In Stock | |
| 25 mg | $1,590 | In Stock | In Stock | |
| 50 mg | $2,580 | In Stock | In Stock | |
| 1 mL x 10 mM (in DMSO) | $622 | In Stock | In Stock |
| Description | ZED-1227 (TAK-227) is an orally active, selective and potent transglutaminase 2 (TG2) inhibitor with anticancer activity that blocks inflammation-induced TG2 expression and activation for the treatment of Celiac Disease. |
| Targets&IC50 | TGase 2:45 nM |
| In vitro | ZED-1227, at concentrations ranging from 0.1 μM to 1 μM for 24 hours, does not impact metabolic activity and proliferation in Huh7 cells and CaCo2 cells. This lack of effect suggests that ZED-1227 does not exhibit cytotoxic activity[1]. In an in vitro setting, ZED-1227, when applied at concentrations between 0.002 and 0.2 mg/mL for 30 minutes, inhibits transglutaminase 2 (TG2) in the small intestinal mucosa[1]. |
| In vivo | In mice, ZED-1227 reduces the activity of intestinal TG2 induced by Polyinosinic:Polycytidylic acid (40 mg/kg) to levels comparable to normal control levels. Additionally, ZED-1227 administration subdues intestinal inflammation in these mice[1].Furthermore, when administered orally (5 mg/kg; i.g.), ZED-1227 is effective in inhibiting TG2 in the small intestinal mucosa[1]. |
| Synonyms | ZED-101, TAK-227 |
| Molecular Weight | 528.6 |
| Formula | C26H36N6O6 |
| Cas No. | 1542132-88-6 |
| Smiles | CCC(CC)CNC(=O)Cn1cccc(NC(=O)[C@H](CC\C=C\C(=O)OC)NC(=O)c2cncn2C)c1=O |
| Relative Density. | 1.24 g/cm3 (Predicted) |
| Storage | store at low temperature,keep away from direct sunlight | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 100 mg/mL (189.18 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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