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AZD 5248

Cat. No. 7130 提交评论 说明书 / 分析证书（CoA） / 化学品安全技术说明书（SDS）
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说明： Potent cathepsin C inhibitor
化学名： 4-Amino-N-[(1S)-1-cyano-2-(4'-cyano[1,1'-biphenyl]-4-yl)ethyl]tetrahydro-2H-pyran-4-carboxamide
纯度： ≥98% (HPLC)
说明书
引用文献
评论
生物活性 技术数据 溶解性 计算器 说明书 参考文献

生物活性 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.

技术数据 for AZD 5248

分子量 374.44
公式 C22H22N4O2
储存 Store at -20°C
纯度 ≥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

上方提供的技术数据仅供参考。批次相关数据请参见分析证书。

Tocris products are intended for laboratory research use only, unless stated otherwise.

溶解性数据 for AZD 5248

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 37.44 100
ethanol 7.49 20

制备储备液 for AZD 5248

以下数据基于产品分子量 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.

选择批次从而根据批次分子量重新计算:
浓度/溶剂体积/质量 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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参考文献 for AZD 5248

参考文献是支持产品生物活性的出版物。

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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关键词: 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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