AZ084
目录号: PL02389 纯度: ≥99%
CAS No. :929300-19-6
商品编号 规格 价格 会员价 是否有货 数量
PL02389-5mg 5mg ¥3832.73 请登录
PL02389-10mg 10mg ¥5749.09 请登录
PL02389-50mg 50mg ¥17309.09 请登录
PL02389-100mg 100mg 询价 询价
PL02389-200mg 200mg 询价 询价
PL02389-10mM*1mLinDMSO 10mM*1mLinDMSO ¥4216.00 请登录
Medlife所售产品仅用于科学研究(非临床研究),非药品不可食用,不可用于人体或动物的临床诊断和治疗,我们不为个人提供产品及服务。产品COA等资料,可至下方“质量控制”中下载。
中文名称
AZ084
英文名称
AZ084
英文别名
AZ084;BDBM50414978;(5-Aminopyridin-2-yl)-[9-[(2,2-dimethyl-3H-1-benzofuran-4-yl)methyl]-3,9-diazaspiro[5.5]undecan-3-yl]methanone;(5-aminopyridin-2-yl)(9-((2,2-dimethyl-2,3-dihydrobenzofuran-4-yl)methyl)-3,9-diazaspiro[5.5]undecan-3-yl)methanone;CID 16065569;(5-Amino-2-pyridinyl)[9-[(2,3-dihydro-2,2-dimethyl-4-benzofuranyl)methyl]-3,9-diazaspiro[5.5]undec-3-yl]methanone (ACI);AZ 084
Cas No.
929300-19-6
分子式
C26H34N4O2
分子量
434.57
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
AZ084 是一种具有口服活性的选择性 CCR8 的变构拮抗剂,其Ki 值为 0.9 nM。AZ084 可通过下调 Treg 的分化来抑制免疫耐受性 PMN 的形成和肿瘤细胞在肺部的转移。AZ084 可用于哮喘和癌症的研究。
生物活性
AZ084 is a potent, selective, allosteric and oral active CCR8 allosteric antagonist, with a K i of 0.9 nM. Has potential to treat asthma. AZ084 restrains the formation of the immunologically tolerant pre-metastatic niche (PMN) and tumor cells metastasis in lung by downregulating Treg differentiation. AZ084 can be used in studies of asthma and cancer.
性状
Solid
IC50 & Target[1][2]
CCR8 0.9 nM (Ki)
体外研究(In Vitro)
AZ084 (5 μg/mL; single daily for 4 days) suppresses proportion of Tregs and reduces T cells that expresses CCR8 (co-cultured in vitro with LLC-exo MPF CM).
AZ084 (0-10 μM) inhibits AML, DC and T cells with IC50s of 1.3, 4.6 and 5.7 nM, respectively. has not independently confirmed the accuracy of these methods. They are for reference only.Cell Viability Assay
体内研究(In Vivo)
AZ084 (5 mg/kg; i.p.; every third day for 9 or 21 days) restrains the formation of the immunologically tolerant PMN and tumor cells metastasis in lung by downregulating Treg differentiation.
AZ084 (434.57-869.14 mg/kg; i.v.; single) shows a bioavailability >70% in rats. 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
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Wang M, et al. Tumor-derived exosomes drive pre-metastatic niche formation in lung via modulating CCL1+ fibroblast and CCR8+ Treg cell interactions. Cancer Immunol Immunother. 2022 Apr 15.
[2]. Connolly S, et al. Orally bioavailable allosteric CCR8 antagonists inhibit dendritic cell, T cell and eosinophil migration. Biochem Pharmacol. 2012 Mar 15;83(6):778-87.
溶解度数据
In Vitro: DMSO : 250 mg/mL (575.28 mM; Need ultrasonic)配制储备液
搜索质检报告(COA)

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。

The molarity calculator equation
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
The dilution calculator equation
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2