2. GPCR/G Protein Immunology/Inflammation
  3. CCR
  4. ZK 756326

ZK756326 是一种非肽趋化因子受体激动剂，作用于 CC 趋化因子受体 CCR8。

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ZK 756326 Chemical Structure

ZK 756326 Chemical Structure

CAS No. : 874911-96-3

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ZK 756326 的其他形式现货产品:

Customer Review

Other Forms of ZK 756326:

ZK 756326 相关抗体

Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 1 篇科研文献

查看 CCR 亚型特异性产品:

查看所有亚型
CCR1 CCR2 CCR3 CCR4 CCR5 CCR6 CCR7 CCR8 CCR9

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

ZK756326 is a nonpeptide chemokine receptor agonist for the CC chemokine receptor CCR8.

IC50 & Target

IC50: 1.8 μM (CCR8)[1]
体外研究
(In Vitro)

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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

ZK 756326 相关抗体:
分子量

356.46

Formula

C21H28N2O3
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献
Cell Assay
[1]

U87 MG cells expressing CCR8 are plated on poly-D-lysine-coated black 96-well plates at 10,000 cells/well and are cultured overnight. Cells are then loaded with Calcium 3, a Ca2+-sensitive non-wash fluorescence dye, for 60 min at 37°C in Hanks' balanced salts solution containing 20 mM HEPES, 3.2 mM CaCl2, 1% (v/v) fetal bovine serum, and 2.5 mM probenecid. Changes in intracellular free-Ca2+ concentration are measured with Fluorometric Imaging Plate Reader (FLIPR 3) immediately after the addition of agonist at room temperature. Cross-desensitization experiments are performed by a first addition of the agonist (CCL1 at 30 nM or ZK 756326 at 3 μM), immediately followed by a second addition of 100 nM CCL1[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

ZK 756326 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

ZK 756326874911-96-3ZK756326ZK-756326CCRCC chemokine receptorInhibitorinhibitorinhibit

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产品名称：
ZK 756326
目录号：
HY-101038
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