AZD 5248

Pricing Availability   Qty
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
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
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.

Select a batch to recalculate based on the batch molecular weight:
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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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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Citations for AZD 5248

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