AZD 5248
Tocris Bioscience, part of Bio-Techne | Catalog # 7130
Potent cathepsin C inhibitor
Key Product Details
Description
Potent cathepsin C inhibitor
Product Description
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.Product Specifications
Molecular Weight
374.44
Formula
C22H22N4O2
Storage
Store at -20°C
Purity
≥98% (HPLC)
Chemical Name
4-Amino-N-[(1S)-1-cyano-2-(4'-cyano[1,1'-biphenyl]-4-yl)ethyl]tetrahydro-2H-pyran-4-carboxamide
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.
Solubility
| 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 all 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 |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
References are publications that support the biological activity of the product.
- Bragg Aortic binding of AZD5248: mechanistic insight and reactivity assays to support lead optimization. Chem.Res.Toxicol. 2015 PMID: 26351880
- Furber Cathepsin C inhibitors: property optimization and identification of a clinical candidate. J.Med.Chem. 2014 PMID: 24592859
- Gardiner Neutrophil maturation rate determines the effects of dipeptidyl peptidase 1 inhibition on neutrophil serine protease activity. Br.J.Pharmacol. 2016 PMID: 27186823
Product Specific Notices for AZD 5248
For research use only
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