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Human GCGR (Luc) HEK293 Reporter Cell

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CHEK-ATF103-2Vials (1Vial X 2)
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产品详情

    1. Genetically modified cell lines best reflect MOA (Mechanism of Action)
    2. Higher activity and larger assay window for robust and reproducible cell-based bioassay
    3. Comprehensive application data to support assay development and validation
    4. Full tracible record, stringent quality control and validated cell passage stability
    5. Parental cell line legally obtained from internationally recognized cell resource bank and commercially licensed
    6. Global commercial license assistance whenever regulatory filing is required

  • 描述（Description）

    The Human GCGR (Luc) HEK293 Reporter Cell was engineered to not only express CREB signaling response element, but also express the receptor full length human GCGR (Gene ID: 2642), which can drive luciferase expressing systems by GCGR agonists or Glucagon stimulation. In the absence of agonist or Glucagon, the GCGR receptor is not activated and luminescence signal is low. In the presence of agonist or Glucagon, the GCGR pathway-activated luminescence can be detected in a dose-dependent manner.

  • 应用说明（Application）

    • Screen for agonists that can bind and activate GCGR.

    GCGR Assay Principles

  • 生长特性（Growth Properties）

    Adherent

  • 筛选标记（Selection Marker）

    Puromycin (2 μg/mL) + Hygromycin (20 μg/mL)

  • 培养基（Complete Growth Medium）

    DMEM medium + 10% FBS

  • 冻存液（Freeze Medium）

    Serum-free cell cryopreservation medium

  • 装量（Quantity）

    1 vial contains at least 5×10^6 cells in 1 mL serum-free cryopreservation medium

  • 存储（Storage）

    Frozen in liquid nitrogen.

  • 支原体检测（Mycoplasma Testing）

    Negative

  • 无菌检测（Sterility Testing）

    Negative

  • 使用说明（Instructions for Use）

    See data sheet for detailed culturing and assay protocol.

数据展示

  • Receptor Assay

    GCGR FACS

    Expression analysis of human GCGR on Human GCGR (Luc) HEK293 Reporter Cell by FACS.
    Cell surface staining was performed on Human GCGR (Luc) HEK293 Reporter Cell or negative control cell using Alexa Fluor® 488-labeled anti-human GCGR antibody.

    Protocol

  • Application

    GCGR APPLICATION

    Bioactivity analysis of human GCGR agonist (RLU).
    This reporter cell was incubated with serial dilutions of Retatrutide (a triple agonist peptide of GCGR, GIPR and GLP-1R). The EC50 of Retatrutide was approximately 0.024 nM.

    Protocol

  • GCGR APPLICATION

    Bioactivity analysis of human GCGR agonist (FOLD).
    This reporter cell was incubated with serial dilutions of Retatrutide (a triple agonist peptide of GCGR, GIPR and GLP-1R). The max induction fold was approximately 79.93.

    Protocol

  • Passage Stability

    GCGR PASSAGE

    Passage stability analysis by Signaling Bioassay.
    The continuously growing Human GCGR (Luc) HEK293 Reporter Cell was stimulated with serial dilutions of Retatrutide (a triple agonist peptide of GCGR, GIPR and GLP-1R). Retatrutide stimulated response demonstrates passage stabilization (fold induction and EC50) across passage 7-20.

    Protocol
*如有相关细胞池需求请联系我们

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背景介绍

G-protein coupled receptor for glucagon that plays a central role in the regulation of blood glucose levels and glucose homeostasis. Regulates the rate of hepatic glucose production by promoting glycogen hydrolysis and gluconeogenesis. Plays an important role in mediating the responses to fasting. Ligand binding causes a conformation change that triggers signaling via guanine nucleotide-binding proteins (G proteins) and modulates the activity of down-stream effectors, such as adenylate cyclase. Promotes activation of adenylate cyclase. Besides, plays a role in signaling via a phosphatidylinositol-calcium second messenger system.

前沿进展

 
药物研发进展
  • 英文全称：

    Glucagon receptor

  • 中文全称：

    胰高血糖素受体

  • 种类：

  • 上市药物数量：

    5 详情

  • 临床药物数量：

    30 详情

  • 最高研发阶段：

    批准上市

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  • 产品详情
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