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首页-小分子抑制剂&激动剂-GPCR-Chemokine Receptor (CCR and CXCR)-AZD 5069
AZD 5069

Chemical Structure : AZD 5069

CAS No.: 878385-84-3

AZD 5069 (AZD5069;AZD-5069)

货号: PC-60618Not For Human Use, Lab Use Only.

AZD 5069 (AZD5069) is a potent, selective, slowly reversible and orally bioavailable CXCR2 antagonist that inhibits CXCL8 binding to CXCR2 with pIC50 of 9.1.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

AZD 5069 (AZD5069) is a potent, selective, slowly reversible and orally bioavailable CXCR2 antagonist that inhibits CXCL8 binding to CXCR2 with pIC50 of 9.1.
AZD5069 weakly inhibits CXCL8 binding to CXCR1 with pIC50<7, and no affinity for CCR2 and CCR5.
AZD5069 inhibits neutrophil chemotaxis with pA2 of 9.6, and adhesion molecule expression of 6.9, in response to CXCL1.
AZD5069 demonstrates potential activity in acute LPS-induced lung inflammation models.

物理化学性质&存储条件

分子量 476.51
分子式 C18H22F2N4O5S2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

N-(2-((2,3-difluorobenzyl)thio)-6-(((2R,3S)-3,4-dihydroxybutan-2-yl)oxy)pyrimidin-4-yl)azetidine-1-sulfonamide

参考文献

1. Nicholls DJ, et al. J Pharmacol Exp Ther. 2015 May;353(2):340-50.

2. Jurcevic S, et al. Br J Clin Pharmacol. 2015 Dec;80(6):1324-36.

3. Kirsten AM, et al. Pulm Pharmacol Ther. 2015 Apr;31:36-41.

4. Walters I, et la. Bioorg Med Chem Lett. 2008 Jan 15;18(2):798-803.

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