AZD 5248

Name: AZD 5248
Brand: Tocris Bioscience
SKU: 7130

Tocris Bioscience, part of Bio-Techne | Catalog # 7130

COA / SDS

Potent cathepsin C inhibitor

Key Product Details

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)
Molecular Weight:	374.44

View Full Technical Details for AZD 5248

Technical Data
Citations

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 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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References for AZD 5248

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