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AZ084

カタログ番号GC65213 Copy One-Click Copy Product Info

AZ084 は、0.9 nM の Ki を持つ強力な選択的アロステリックおよび経口活性 CCR8 アロステリック アンタゴニストです。

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AZ084 化学構造

Cas No.: 929300-19-6

サイズ 価格 在庫数 個数
10mM (in 1mL DMSO)
$165.00
在庫あり
1mg
$73.00
在庫あり
5mg
$172.00
在庫あり
10mg
$261.00
在庫あり
25mg
$422.00
在庫あり

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顧客レビュー

カスタマーレビューに基づきます。

Sample solution is provided at 25 µL, 10mM.



Description of AZ084

AZ084 is a potent, selective, allosteric and oral active CCR8 allosteric antagonist, with a Ki of 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 downregulating Treg differentiation. AZ084 can be used in studies of asthma and cancer[1][2].

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].

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].

[1]. 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.

Protocol of AZ084

CCR8

0.9nM(Ki)

Chemical Properties of AZ084

Cas No. 929300-19-6 SDF
Formula C26H34N4O2 M.Wt 434.57
溶解度 DMSO : 250 mg/mL (575.28 mM; Need ultrasonic) Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of AZ084

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 2.3011 mL 11.5056 mL 23.0113 mL
5 mM 460.2 μL 2.3011 mL 4.6023 mL
10 mM 230.1 μL 1.1506 mL 2.3011 mL
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Average Rating: 5 ★★★★★ (Based on Reviews and 30 reference(s) in Google Scholar.)

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