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Human GLP-1R (Luc) HEK293 Reporter Cell

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CHEK-ATF096-2Vials (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 GLP-1R (Luc) HEK293 Reporter Cell was engineered to not only express CREB signaling response element, but also express the receptor full length human GLP-1R (Gene ID: 2740), which can drive luciferase expressing systems by GLP-1R agonists or glucagon-like peptide 1(GLP-1) stimulation. In the absence of agonist or GLP-1, the GLP-1R receptor is not activated and luminescence signal is low. In the presence of agonist or GLP-1, the GLP-1R pathway-activated luminescence can be detected in a dose-dependent manner.

  • 应用说明（Application）

    • Screen for agonists that can bind and activate GLP-1R

    GLP1R 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

    GLP1R FACS

    Expression analysis of human GLP-1R on Human GLP-1R (Luc) HEK293 Reporter Cell by FACS.
    Cell surface staining was performed on Human GLP-1R (Luc) HEK293 Reporter Cell or negative control cell using PE-labeled anti-human GLP-1R antibody.

    Protocol

  • Application

    GLP1R APPLICATION

    Bioactivity analysis of human GLP-1R agonist (RLU).
    This reporter cell was incubated with serial dilutions of Tirzepatide (a dual GLP-1R and GIPR agonist). The EC50 of Tirzepatide was approximately 1.11 nM.

    Protocol

  • GLP1R APPLICATION

    Bioactivity analysis of human GLP-1R agonist (FOLD).
    This reporter cell was incubated with serial dilutions of Tirzepatide (a dual GLP-1R and GIPR agonist). The max induction fold was approximately 334.81.

    Protocol

  • Passage Stability

    GLP1R PASSAGE

    Passage stability analysis by Signaling Bioassay.
    The continuously growing Human GLP-1R (Luc) HEK293 Reporter Cell was stimulated with serial dilutions of Tirzepatide (a dual GLP-1R and GIPR agonist). Tirzepatide stimulated response demonstrates passage stabilization (fold induction and EC50) across passage 8-24.

    Protocol
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背景介绍

This gene encodes a 7-transmembrane protein that functions as a receptor for glucagon-like peptide 1 (GLP-1) hormone, which stimulates glucose-induced insulin secretion. This receptor, which functions at the cell surface, becomes internalized in response to GLP-1 and GLP-1 analogs, and it plays an important role in the signaling cascades leading to insulin secretion. It also displays neuroprotective effects in animal models. Polymorphisms in this gene are associated with diabetes. The protein is an important drug target for the treatment of type 2 diabetes and stroke.

前沿进展

 
药物研发进展
  • 英文全称：

    Glucagon-like peptide-1

  • 中文全称：

    胰高血糖素类肽-1

  • 种类：

  • 上市药物数量：

    0 详情

  • 临床药物数量：

    5 详情

  • 最高研发阶段：

    临床三期

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