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AZD-4818 Sale

目录号 : GC63284

AZD-4818 是趋化因子 CCR1 的有效拮抗剂。AZD-4818 可用于治疗慢性阻塞性肺病 (COPD)。

AZD-4818 Chemical Structure

Cas No.:1003566-93-5

规格 价格 库存 购买数量
5 mg
¥2,250.00
现货
10 mg
¥4,050.00
现货
25 mg
¥8,550.00
现货

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Sample solution is provided at 25 µL, 10mM.

产品文档

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产品描述

AZD-4818 is a potent antagonist of chemokine CCR1. AZD-4818 can be used for the treatment of chronic obstructive pulmonary disease (COPD) [1].

[1]. Norman P. AZD-4818, a chemokine CCR1 antagonist: WO2008103126 and WO2009011653. Expert Opin Ther Pat. 2009;19(11):1629-1633.

Chemical Properties

Cas No. 1003566-93-5 SDF
分子式 C27H32Cl2N2O7 分子量 567.46
溶解度 DMSO : 50 mg/mL (88.11 mM; ultrasonic and adjust pH to 2 with HCl) 储存条件 Store at -20°C
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溶解性数据

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1 mg 5 mg 10 mg
1 mM 1.7622 mL 8.8112 mL 17.6224 mL
5 mM 0.3524 mL 1.7622 mL 3.5245 mL
10 mM 0.1762 mL 0.8811 mL 1.7622 mL
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Research Update

AZD-4818, a chemokine CCR1 antagonist: WO2008103126 and WO2009011653

Expert Opin Ther Pat 2009 Nov;19(11):1629-33.PMID:19586423DOI:10.1517/13543770903118996.

The applications WO2008103126 and WO2009011653, respectively, claim: i) Combinations of a spirocyclic piperidine chemokine CCR1 antagonist with a corticosteroid, and their use for the treatment of asthma and chronic obstructive pulmonary disease. ii) Processes for the preparation of a spirocyclic piperidine derivative, a chemokine CCR1 antagonist. These applications point to the preferred compound being a development compound. The evidence for this compound being AZD-4818, a chemokine CCR1 antagonist that was in Phase II development for the treatment of chronic obstructive pulmonary disease, is reviewed in the light of these and earlier patents relating to it.

CCR1 antagonists: what have we learned from clinical trials

Curr Top Med Chem 2010;10(13):1268-77.PMID:20536425DOI:10.2174/156802610791561237.

The identification of chemokines and their receptors as potent mediators of leukocyte infiltration raised interest in the potential role of these proteins on disease pathogenesis. This is exemplified by the chemokine receptor, CCR1, which has been shown to be up-regulated in a number of human diseases, the implications of which have been suggested by animal models where inhibition of CCR1 or its ligands have shown beneficial effects. These data support the possibility that a CCR1 antagonist will provide therapeutic benefit to patients with inflammatory diseases. Over the last several years, several of these antagonists entered clinical trials, including CP-481,715 (Pfizer) and MLN3897 (Millennium) for rheumatoid arthritis, BX471 (Berlex / Scherring AG) for multiple sclerosis, and AZD-4818 (Astra-Zeneca) for COPD. This review will describe the evidence that supported the role of CCR1 in these diseases, the results from clinical trials, and provide perspectives on what has been learned from these trials for potential application / consideration to other studies with chemokine receptor antagonists.