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AZD9056 hydrochloride

目录号: PL08676 纯度: ≥98%

AZD9056 hydrochloride 是具有口服活性的P2X7选择性抑制剂，其在炎症和引起疼痛的疾病中起重要作用。

CAS No. :345303-91-5

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PL08676-1 mL x 10 mM (in DMSO)		¥593.00	请登录

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中文名称	AZD9056 hydrochloride
中文别名	AZD9056 (hydrochloride)
英文名称	AZD9056 hydrochloride
英文别名	AZD9056 (hydrochloride);AZD9056 hydrochloride;AZD-9056 hydrochloride
Cas No.	345303-91-5
分子式	C₂₄H₃₆Cl₂N₂O₂
分子量	455.46
包装储存	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
详情描述	AZD9056 hydrochloride 是具有口服活性的P2X7选择性抑制剂，其在炎症和引起疼痛的疾病中起重要作用。

产品详情

AZD9056 hydrochloride 是具有口服活性的P2X7选择性抑制剂，其在炎症和引起疼痛的疾病中起重要作用。

生物活性

AZD9056 hydrochloride is a selective orally active inhibitor of P2X7 which plays a significant role in inflammation and pain-causing diseases.

性状

Solid

IC50 & Target[1][2]

P2X7 Receptor

体外研究(In Vitro)

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). has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

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. has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

ClinicalTrial

参考文献

[1]. Seeland S, et al. ATP-induced cellular stress and mitochondrial toxicity in cells expressing purinergic P2X7 receptor. Pharmacol Res Perspect. 2015 Mar;3(2):e00123.
[2]. Elsby R, et al. In vitro risk assessment of AZD9056 perpetrating a transporter-mediated drug-drug interaction with methotrexate. Eur J Pharm Sci. 2011 May 18;43(1-2):41-9.

溶解度数据	In Vitro: DMSO : 50 mg/mL (109.78 mM; Need ultrasonic)H₂O : 1.67 mg/mL (3.67 mM; ultrasonic and warming and heat to 60°C)配制储备液

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

AZD9056 hydrochloride

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