AZ084是一种具有口服活性的选择性 CCR8 变构拮抗剂,Ki 值为 0.9 nM,可通过下调 Treg 的分化抑制免疫耐受性 PMN 的形成及肿瘤细胞在肺部的转移,可用于研究哮喘和癌症。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
50μL*10mM(DMSO) | ¥159 | 咨询 | |
100μL*10mM(DMSO) | ¥249 | 咨询 | |
250μL*10mM(DMSO) | ¥499 | 咨询 | |
500μL*10mM(DMSO) | ¥829 | 咨询 | |
10mM*1mL(DMSO) | ¥1280 | 咨询 | |
1mg | ¥567 | 咨询 | |
5mg | ¥1339 | 咨询 | |
10mg | ¥2030 | 咨询 |
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描述 | AZ084 is a potent, selective, allosteric and orally active CCR8 antagonist with a Ki of 0.9 nM [1].AZ084 inhibits the formation of immunologically tolerant pre-metastatic niche (PMN) and metastasis of tumour cells in the lungs through down-regulation of Treg differentiation [1][2].Administered once daily for 4 days at a concentration of 5 μg/mL, AZ084 inhibits the proportion of Treg and reduces CCR8-expressing T cells (cultured ex vivo with LLC-exo MPF CM)[1][2].At concentrations of 0-10 μM, AZ084 inhibited AML, DC and T cells with IC50 values of 1.3 nM, 4.6 nM and 5.7 nM, respectively[2] . |
Animal study | Administered intraperitoneally at a dose of 5 mg/kg every three days for 9 or 21 days, AZ084 inhibited the formation of immunologically tolerant pre-metastatic niche and metastasis of lung tumour cells by down-regulating Treg differentiation[1] .The bioavailability of AZ084 in rats is greater than 70%[2]. |
计算器 | ||||
存储液制备 | ![]() | 1mg | 5mg | 10mg |
1 mM 5 mM 10 mM | 2.30mL 0.46mL 0.23mL | 11.51mL 2.30mL 1.15mL | 23.01mL 4.60mL 2.30mL |
CAS号 | 929300-19-6 |
分子式 | C26H34N4O2 |
分子量 | 434.574 |
别名 | |
运输 | 蓝冰 |
存储条件 | In solvent -20°C:3-6个月-80°C:12个月 Pure form Keep in dark place,Sealed in dry,2-8°C |
溶解方案 | DMSO: 250 mg/mL(575.28 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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动物实验配方 |