AZD-9056 hydrochloride

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效的、选择性的、口服生物可利用的 P2X7 受体拮抗剂；抑制分离的人外周单核细胞（IL-1β和IL-18）和人肺泡巨噬细胞（IL-1β）释放促炎介质，IC50值为10-13 nM；显示出比其他 P2X 受体 >100 倍的选择性和特异性；也是 BCRP 抑制剂，并弱抑制 BCRP 介导的甲氨蝶呤转运 (IC50=92 uM)；显着降低链球菌细胞壁 (SCW) 关节炎模型的疾病严重程度。

A potent, selective, orally bioavailable P2X7 receptor antagonist; inhibits release of pro-inflammatory mediators from isolated human peripheral monocytes (IL-1β and IL-18) and human alveolar macrophages (IL-1β) with IC50 values of 10-13 nM; displays >100-fold selectivity and specificity other P2X receptors; also is an inhibitor of BCRP and weakly inhibited BCRP-mediated transport of methotrexate (IC50=92 uM); significantly reduces disease severity in the streptococcal cell wall (SCW) model of arthritis.Rheumatoid Arthritis Phase 2 Clinical.

The antagonist AZD9056 blocks P2X7 receptors with an IC50 of 11.2 nM in HEK-hP2X7 cell line, indicating a high selectivity of the antagonist for the P2X7 receptor. The P2X7-receptor antagonist AZD9056 has a clear inhibitory effect (IC50=1-3 μM) in mouse microglia BV2 cells. AZD9056 is an inhibitor of BCRP and weakly inhibits BCRP-mediated transport of methotrexate (IC50=92 μM).

Treatment with AZD9056 exerts pain-relieving and anti-inflammatory effects. The upregulated expression of interleukin (IL)-1β, IL-6, tumor necrosis factor-α (TNF-α), matrix metalloproteinase-13 (MMP-13), substance P (SP) and prostaglandin E2 (PGE2) which is induced by MIA in cartilage tissues is reversed by AZD9056.

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Membrane Transporter/Ion Channel

P2X Receptor

P2X Receptor

Inflammation/Immunology

Rheumatoid Arthritis

345303-91-5

455.46084

C24H36Cl2N2O2

>98% (HPLC)

DMSO: ≥ 34 mg/mL

C1C2CC3CC1CC(C2)(C3)CNC(=O)C4=C(C=CC(=C4)CCCNCCCO)Cl.Cl

Benzamide, 2-chloro-5-[3-[(3-hydroxypropyl)amino]propyl]-N-(tricyclo[3.3.1.13,7]dec-1-ylmethyl)-, hydrochloride (1:1)

(-20℃)

With Ice Pack

≥ 2 years