您好，欢迎来到化工原料网！ [登录] [免费注册]
化工原料网
发布求购
位置：首页 > 产品库 > AZ084
立即咨询
咨询类型：
     
*姓名：
*电话：
*单位：
Email：
*留言内容：
请详细说明您的需求。
*验证码：
 
AZ084
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
AZ084图片
CAS NO:929300-19-6
包装与价格：
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
50mg电议
100mg电议
200mg电议

产品介绍
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 activeCCR8allosteric antagonist, with aKiof 0.9 nM. Has potential to treat asthma[1]. AZ084 restrains the formation of the immunologically tolerant pre-metastatic niche (PMN) and tumor cells metastasis in lung by downregulatingTregdifferentiation. AZ084 can be used in studies of asthma andcancer[1][2].

IC50& Target[1]

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)[1].
AZ084 (0-10 μM) inhibits AML, DC and T cells with IC50s of 1.3, 4.6 and 5.7 nM, respectively[2].

Cell Viability Assay[1]

Cell Line:Splenic T cells
Concentration:5 μg/mL (single daily)
Incubation Time:4 days
Result:Reversed the increased proportion of Tregs among the CD4+ T cells co-cultured in vitro with LLC-exo MPF CM.
Reduced T cells that expressed CCR8 (cultured in vitro with by LLC-exo MPF CM).

Cell Viability Assay[2]

Cell Line:AML, DC and T cells
Concentration:0-10 μM
Incubation Time:
Result:Showed high potency with pronounced dose-response dependent inhibition of chemotaxis with an IC50of 1.3 nM in AML cells.
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[1].
AZ084 (434.57-869.14 mg/kg; i.v.; single) shows a bioavailability >70% in rats[2].

Animal Model:C57BL/6 J mice (subcutaneous LLC tumor model)[1].
Dosage:5 mg/kg
Administration:Intraperitoneal injection, every third day for 9 or 21 days.
Result:Inhibited Treg differentiation and tumor cell colonization of the lungs and reduced the number of CD4+Foxp3+ Tregs in the lungs of LLC-exo pre-injected mice (every third day for 9 days).
Inhibited the LLC-exo-induced LLC cell seeding in lung and also significantly reduced Treg accumulation in LLC-exo stimulated mouse lungs(every third day for 21 days).
Animal Model:Female Balb/C mice, male Wistar rats and female Beagle dogs[2].
Dosage:434.57-869.14 mg/kg (in 0.9% NaCl)
Administration:Intravenous injection, single.
Result:1.19Pharmacokinetic Parameters of AZ084 in Female Balb/C mice, male Wistar rats and female Beagle dogs[2].
IV (434.57-869.14 mg/kg)
Dog plasma protein binding (% free)45.7
Mu plasma protein binding (% free)55.6
Hu plasma protein binding (% free)31.0
Rat plasma protein binding (% free)47.0
Rat HW plasma PK CL (mL/min/kg)15.0
Rat HW plasma PK Vss(L/kg)6.0
Rat HW plasma PK T1/2(h)5.4
Rat HW plasma PK Cmax(μM)0.5
Rat HW plasma PK bioavailability (%)68.0
分子量

434.57

性状

Solid

Formula

C26H34N4O2

CAS 号

929300-19-6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : 250 mg/mL(575.28 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.3011 mL11.5056 mL23.0113 mL
5 mM0.4602 mL2.3011 mL4.6023 mL
10 mM0.2301 mL1.1506 mL2.3011 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro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，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制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

  • 1.

    请依序添加每种溶剂： 10% DMSO    40%PEG300   5%Tween-80   45% saline

    Solubility: ≥ 2.08 mg/mL (4.79 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.79 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH2O 中，得到澄清透明的生理盐水溶液
  • 2.

    请依序添加每种溶剂： 10% DMSO    90% (20%SBE-β-CDin saline)

    Solubility: ≥ 2.08 mg/mL (4.79 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.79 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
  • 3.

    请依序添加每种溶剂： 10% DMSO    90%corn oil

    Solubility: ≥ 2.08 mg/mL (4.79 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.79 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在本网站选购。