| CAS NO: | 901751-47-1 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| 250mg | 电议 |
| 500mg | 电议 |
| Molecular Weight (MW) | 394.53 |
|---|---|
| Formula | C23H26N2O2S |
| CAS No. | 901751-47-1 |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility (In vitro) | DMSO: 80 mg/mL |
| Water: < 1 mg/mL | |
| Ethanol: 80 mg/mL | |
| Chemical Name | 2-[[[2-(4-ethylphenyl)-5-methyl-4-oxazolyl]methyl]thio]-N-(2-phenylethyl)acetamide |
| Synonyms | iCRT 3 |
| SMILES Code | O=C(NCCC1=CC=CC=C1)CSCC2=C(C)OC(C3=CC=C(CC)C=C3)=N2 |
| In Vitro | In vitro activity: iCRT3 is a potent small molecule inhibitor of the Wnt pathway that binds to β-catenin interferes with its interaction with TCF. iCRT3 significantly reduces the LPS-induced Wnt/β-catenin activity and also inhibits TNF-α production and IκB degradation in a dose-dependent manner. iCRT3 does not influence the transcriptional activity of FOP-Flash luciferase reporter, which harbors mutations in the DNA binding sites for TCF (β-cat response element), showing specificity of the response. It inhibits cytokine production in LPS-stimulated macrophages. Kinase Assay: iCRT3 is an inhibitor of Wnt/β-catenin signaling with an IC50 of 8.2 nM in the Wnt responsive STF16-luc reporter assays. Cell Assay: cells (HCT116) were cultured in McCoy's 5A medium supplemented with 10% FBS. Cells were treated with specified concentrations of compounds for 1 d and lysed in 50 μL cell lysis buffer at 75℃ for 10 min. |
|---|---|
| In Vivo | I.P. injection of iCRT3 to C57BL/6 mice, subjected to cecal ligation and puncture-induced sepsis, decreases the plasma levels of proinflammatory cytokines and organ injury markers in a dose-dependent manner. The histological integrity of the lungs is improved with iCRT3 treatment, along with reduced lung collagen deposition and apoptosis. In addition, iCRT3 treatment also decreases the expression of the cytokines, neutrophil chemoattractants, as well as the MPO activity in the lungs of septic mice. |
| Animal model | C57BL/6 mice |
| Formulation & Dosage | Dissolved in 5% DMSO in saline; 5 and 10 mg/kg; i.p. |
| References | Sci Rep. 2017 Aug 23;7(1):9235; Proc Natl Acad Sci U S A. 2011 Apr 12;108(15):5954-63. |
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