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Description: Potent cathepsin C inhibitor
Chemical Name: 4-Amino-N-[(1S)-1-cyano-2-(4'-cyano[1,1'-biphenyl]-4-yl)ethyl]tetrahydro-2H-pyran-4-carboxamide
Purity: ≥98% (HPLC)
Biological Activity for AZD 5248
AZD 5248 is a potent cathepsin C (also known as dipeptidyl peptidase 1, or DPP1) inhibitor (IC50 values are 44 and 67 nM for human and rat, respectively). In vivo, AZD 5248 inhibition of cathepsin C correlates to the reduction of NSP (neutrophil serine protease) activity measured in rat bone marrow and blood. In rats, quantitative whole-body autoradiography studies demonstrate aortic binding of AZ 5248. This compound is orally bioavailable.
Technical Data for AZD 5248
| M. Wt | 374.44 |
| Formula | C22H22N4O2 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1254318-44-9 |
| PubChem ID | 49783666 |
| InChI Key | NNUFRZJZOXVZIT-FQEVSTJZSA-N |
| Smiles | NC1(C(N[C@H](C#N)CC2=CC=C(C3=CC=C(C#N)C=C3)C=C2)=O)CCOCC1 |
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 AZD 5248
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 37.44 | 100 | |
| ethanol | 7.49 | 20 |
Preparing Stock Solutions for AZD 5248
The following data is based on the product molecular weight 374.44. 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 | 2.67 mL | 13.35 mL | 26.71 mL |
| 5 mM | 0.53 mL | 2.67 mL | 5.34 mL |
| 10 mM | 0.27 mL | 1.34 mL | 2.67 mL |
| 50 mM | 0.05 mL | 0.27 mL | 0.53 mL |
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Product Datasheets for AZD 5248
References for AZD 5248
References are publications that support the biological activity of the product.
Gardiner et al (2016) Neutrophil maturation rate determines the effects of dipeptidyl peptidase 1 inhibition on neutrophil serine protease activity. Br.J.Pharmacol. 173 2390 PMID: 27186823
Bragg et al (2015) Aortic binding of AZD5248: mechanistic insight and reactivity assays to support lead optimization. Chem.Res.Toxicol. 28 1991 PMID: 26351880
Furber et al (2014) Cathepsin C inhibitors: property optimization and identification of a clinical candidate. J.Med.Chem. 57 2357 PMID: 24592859
If you know of a relevant reference for AZD 5248, please let us know.
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Keywords: AZD 5248, AZD 5248 supplier, AZD5248, cathepsin, C, inhibitors, inhibits, potent, orally, bioavailable, DDP1, Dipeptidyl, Peptidase, 1, proteases, Cathepsin, 7130, Tocris Bioscience
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