1. PROTAC Neuronal Signaling GPCR/G Protein
  2. Molecular Glues Adrenergic Receptor
  3. AP-7-168

AP-7-168,分子胶,是一种 β-抑制蛋白偏向性的 β2 肾上腺素受体 (β2-adrenergic receptor) 负性变构调节剂。AP-7-168 可促进 β2AR 同源二聚化,并抑制 GRK5 介导的 β2AR 磷酸化。AP-7-168 能维持细胞和组织中支气管舒张。AP-7-168 可用于炎症和免疫学研究,如哮喘研究。

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AP-7-168

AP-7-168 Chemical Structure

CAS No. : 2816062-15-2

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生物活性

AP-7-168, molecular glues, is a β-arrestin-biased negative allosteric modulator of the β2-adrenergic receptor (β2AR). AP-7-168 can promote β2AR homodimerization and inhibit GRK5-mediated β2AR phosphorylation. AP-7-168 can sustain bronchorelaxation in cell and tissue. AP-7-168 can be used for the researches of inflammation and immunology, such as asthma[1].

IC50 & Target[1]

Beta-2 adrenergic receptor

 

体外研究
(In Vitro)

AP-7-168 (0.03-100 μM, 1 h) 可促进 HEK293 细胞中 β2AR 同源二聚化,其 pEC50 值为 5.93[1]
AP-7-168 (10 μM) 可抑制表达 β2AR 的细胞中 β-抑制蛋白 2 的募集以及 GRK5 介导的 β2AR 磷酸化[1]

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

分子量

433.29

Formula

C20H19BrF2N4

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
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  • 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.

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产品名称:
AP-7-168
目录号:
HY-179226
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