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ZK 756326,非肽CCR8激动剂

    
98%

ZK756326(dihydrochloride)

源叶(MedMol)
S83985 一键复制产品信息
1780259-94-0
C21H30Cl2N2O3
429.3805
ZK756326(dihydrochloride);ZK756326(dihydrochloride)
货号 规格 价格 上海 北京 珠海 重庆 武汉 购买数量
S83985-10mg促销
98%

¥720.00 ¥570.00

10 - - - -
S83985-50mg促销
98%

¥3090.00 ¥2470.00

10 - - - -
S83985-250mg促销
98%

¥5150.00 ¥4110.00

货期:3-5天 - - - -
产品介绍 参考文献 质检证书(COA) 摩尔浓度计算器 相关产品
产品描述: ZK756326 dihydrochloride is a nonpeptide chemokine receptor agonist for the CC chemokine receptor CCR8.
靶点: CCR8:1.8 μM (IC50, in U87 cells);5-HT1A:5.4 μM (IC50);5-HT2B:4.4 μM (IC50);5-HT2C:34.8 μM (IC50);5-HT5A:16 μM (IC50);5-HT6:5.9 μM (IC50);α2A:<20 μM (IC50)
体外研究: ZK 756326 inhibits the binding of the CCR8 ligand I-309 (CCL1), with an IC50 value of 1.8 μM. ZK 756326 is a full agonist of CCR8, dose-responsively eliciting an increase in intracellular calcium and cross-desensitizing the response of the receptor to CCL1. ZK 756326 stimulates extracellular acidification in cells expressing human CCR8. Binding competition assays are performed on a series of other G-protein-coupled receptors to determine whether the interaction of ZK 756326 is specific for CCR8. In these assays, ZK 756326 is tested at 50 μM for inhibition of radiolabeled ligand binding. At this concentration, ZK 756326 shows >28 fold specificity for CCR8 compared with 26 other GPCRs, all with IC50 values of >50 μM. There is less selectivity when ZK 756326 is tested against the serotonergic receptors 5-HT1A, 5-HT2B, 5-HT2C, 5-HT5A, 5-HT6, and the adrenergic receptor α2A, in which IC50 values of 5.4, 4,4, 34.8, 16, 5.9, and <20 μM (at 20 μM 65% inhibition), respectively, are observed. The compound is unlikely to be an agonist on these biogenic amine receptors, because when tested at concentrations up to 10 μM on a representative receptor, 5-HT1A, it shows no agonist activity in a GTPγS binding assay
参考文献: 1. Haskell CA, et al. Identification and characterization of a potent, selective nonpeptide agonist of the CC chemokine receptor CCR8. Mol Pharmacol. 2006 Jan;69(1):309-16.
溶解性: Soluble  in  DMSO、H2O
保存条件: 2-8℃;干燥
配置溶液浓度参考:
1mg 5mg 10mg
1 mM 2.329 ml 11.645 ml 23.289 ml
5 mM 0.466 ml 2.329 ml 4.658 ml
10 mM 0.233 ml 1.164 ml 2.329 ml
50 mM 0.047 ml 0.233 ml 0.466 ml
注意: 部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。

参考文献

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摩尔浓度计算器

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