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Submit ReviewRAGE 229
Description: ctRAGE-DIAPH1 interaction antagonist; reduces inflammatory signaling in diabetic mice
Chemical Name: N-[4-[7-Cyano-4-(4-morpholinylmethyl)-2-quinolinyl]phenyl]acetamide
Purity: ≥98% (HPLC)
Biological Activity for RAGE 229
RAGE 229 is an antagonist of the interaction between the cytoplasmic tail of the receptor for advanced glycation end products (ctRAGE) and the formin, Diaphanous-1 (DIAPH1) (KD for binding to ctRAGE = 2 nM). RAGE 229 inhibits the migration of human aortic smooth muscle cells in an in vitro wound healing assay (IC50 = 120 nM). RAGE 229 reduces short- and long-term complications of diabetes in mouse models, without lowering blood glucose concentrations. RAGE 229 also reduces plasma concentrations of TNF-α, IL-6, and CCL2/JE-MCP1 and attenuates inflammatory signaling in diabetic mice.
Licensing Information
Sold under license from New York University
Technical Data for RAGE 229
| M. Wt | 386.45 |
| Formula | C23H22N4O2 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 2143072-85-7 |
| PubChem ID | 132020228 |
| InChI Key | VDYYVNHJRNDKDO-UHFFFAOYSA-N |
| Smiles | N#CC=1C=CC=2C(=NC(=CC2CN3CCOCC3)C=4C=CC(=CC4)NC(=O)C)C1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for RAGE 229
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 38.65 | 100 |
Preparing Stock Solutions for RAGE 229
The following data is based on the product molecular weight 386.45. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.59 mL | 12.94 mL | 25.88 mL |
| 5 mM | 0.52 mL | 2.59 mL | 5.18 mL |
| 10 mM | 0.26 mL | 1.29 mL | 2.59 mL |
| 50 mM | 0.05 mL | 0.26 mL | 0.52 mL |
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Product Datasheets for RAGE 229
References for RAGE 229
References are publications that support the biological activity of the product.
Manigrasso et al (2021) Small-molecule antagonism of the interaction of the RAGE cytoplasmic domain with DIAPH1 reduces diabetic complications in mice. Sci.Transl.Med. 13 eabf7084 PMID: 34818060
If you know of a relevant reference for RAGE 229, please let us know.
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Keywords: RAGE 229, RAGE 229 supplier, RAGE229, inhibitor, inhibits, interaction, receptor, for, advanced, glycation, end, products, RAGE, Diaphanous-1, DIAPH1, type, 1, 2, diabetes, anti-inflammatory, 7701, Tocris Bioscience
Citations for RAGE 229
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