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Product name : AZD-5069
Item : C2467
Price : 200mg, $1250;500mg, $2090; 1g, $2995; 2g, $4395
contact : Send inquiry to: info@acesobio.com
CAS : 878385-84-3
Molecular Weight : 476.52
Formula : C18H22F2N4O5S2
Storage : at -20°C
Additional information : We offer significant discount for bulky quantity order.
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Details:
Description of:AZD-5069(CAS:878385-84-3)
AZD-5069 is a potent and selective CXCR2 antagonist with the potential to inhibit neutrophil migration into the airways in patients with COPD. AZD-5069 was shown to inhibit binding of radiolabeled CXCL8 to human CXCR2 with a pIC50 value of 9.1. Furthermore, AZD5069 inhibited neutrophil chemotaxis, with a pA2 of approximately 9.6, and adhesion molecule expression, with a pA2 of 6.9, in response to CXCL1. AZD5069 was a slowly reversible antagonist of CXCR2 with effects of time and temperature evident on the pharmacology and binding kinetics. AZD-5069 is also potential useful for patient in inflammatory conditions.
AZD-5069 acts as CXCR2 antagonist by inhibition of [125I]-IL-8 binding to human CXCR2 receptors and as inhibitor of GROα-induced Ca2+ flux in human neutrophils loaded with fluo-3 dye[1].

Quality control data:
Quality control by 1H-NMR, 13C-NMR, HPLC and LCMS.
Product will be shipped with supporting analytical data.

REFERENCES


1: De Soyza A, Pavord I, Elborn JS, Smith D, Wray H, Puu M, Larsson B, Stockley 
R. A randomised, placebo-controlled study of the CXCR2 antagonist AZD5069 in 
bronchiectasis. Eur Respir J. 2015 Sep 4. pii: ERJ-00148-2015. doi: 
10.1183/13993003.00148-2015. [Epub ahead of print] PubMed PMID: 26341987.

2: Jurcevic S, Humfrey C, Uddin M, Warrington S, Larsson B, Keen C. The effect of 
a selective CXCR2 antagonist (AZD5069) on human blood neutrophil count and innate 
immune functions. Br J Clin Pharmacol. 2015 Jul 15. doi: 10.1111/bcp.12724. [Epub 
ahead of print] PubMed PMID: 26182832.

3: Nicholls DJ, Wiley K, Dainty I, MacIntosh F, Phillips C, Gaw A, Mårdh CK. 
Pharmacological characterization of AZD5069, a slowly reversible CXC chemokine 
receptor 2 antagonist. J Pharmacol Exp Ther. 2015 May;353(2):340-50. doi: 
10.1124/jpet.114.221358. Epub 2015 Mar 3. PubMed PMID: 25736418.

4: Kirsten AM, Förster K, Radeczky E, Linnhoff A, Balint B, Watz H, Wray H, 
Salkeld L, Cullberg M, Larsson B. The safety and tolerability of oral AZD5069, a 
selective CXCR2 antagonist, in patients with moderate-to-severe COPD. Pulm 
Pharmacol Ther. 2015 Apr;31:36-41. doi: 10.1016/j.pupt.2015.02.001. Epub 2015 Feb 
11. PubMed PMID: 25681277.


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