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G蛋白偶联受体(GPCR)的检测
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GPCR靶点筛选
技术服务 研发实验室
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G Protein-coupled Receptors (GPCRs)

G protein-coupled receptors (GPCRs) are the largest class of membrane proteins in the human genome and they representing the largest family of validated therapeutic targets with over 800 know human GPCRs. The new member’s list is growing daily with advances in new techniques.

About half of GPCRs have sensory functions, mediating olfaction (~400), taste (33), light perception (10) and pheromone signalling. The remaining ~350 non-sensory GPCRs mediate signalling by ligands that range in size from small molecules to peptides to large proteins; they are the targets for the majority of drugs in clinical usage. Over 1500 drugs were approved by the FDA, where around 40% drugs target mainly GPCRs.

To support researchers drug R&D activity, ScreeNingBio encourages exploring all possible signaling scenarios with a variety of available biologically-relevant cell-based functional and binding assays and stable cell lines.

ScreeNingBio’s stable GPCR panel including the full human, mouse and rat GPCRs which are no promiscus G protein co-transfection. The GPCR products in the ScreeNingBio are sensitive and robust for detecting receptor-mediated second messenger signals (cAMP, IP1 and calcium), β-arrestin recruitment, receptor internalization, and ligand binding. These assays are suitable for the compounds profiling and high throughput screening.

cAMP Assays: Homogeneous TR-FRET cAMP detection cell-based assays to monitor the functional status of GPCRs upon small molecules or biologics binding. Characterize ligand pharmacology and obtain reproducible performance with large assay windows and broad sensitivity ranges.

IP1 Assays: Homogeneous TR-FRET IP1 detection cell-based assays to monitor the functional status of GPCRs upon small molecules or biologics binding. Characterize ligand pharmacology and obtain reproducible performance with large assay windows and broad sensitivity ranges.

Calcium Assays: Fluorescent dye-based assays to measure calcium mobilization in cell lines as a direct indication of GPCR activation or inhibition.

β-Arrestin Assays: Universal G-protein independent cell-based assays to quantify GPCR activation based on the recruitment of β-arrestin. Ideal for ligand bias analysis, antagonist mode screening, and studying virtually any GPCR including orphan receptors.

GPCR Internalization Assays: Secondary, orthogonal screening cell-based assays for measuring GPCR desensitization and recycling as well as uncovering novel classes of compound pharmacologies and identifying safer drugs without imaging or antibodies.

Membrane Preparations: Purified membrane preps for obtaining GPCR ligand binding affinities and evaluating GPCR activity through GTPγS functional studies in response to the addition of a ligand or therapeutic.


G蛋白偶联受体(GPCR)是一类重要的治疗靶点,为方便和加速GPCR药物发现及生物学研究,格宁生物(ScreeNingBio)提供高质量的细胞模型和化合物筛选技术服务,包括第二信使激活 (cAMP, IP1, Ca2+)、β-Arrestin、受体内吞等试验。
目前,格宁生物开发了human-, mouse-, rat-等种属的500+GPCR细胞库和筛选平台以适应灵活多样的项目类型——如Compound Profiling和高通量筛选,并可根据合作伙伴的需求提供定制服务。无论采取何种技术平台,格宁生物均可提供可靠和高通量的GPCR检测试验
  构效关系研究(SAR)和高通量筛选(HTS):

      -cAMP HTRF assay (Gαs, Gαi)
      -IP1 HTRF assay (Gαq)
      -Calcium flux assay (Gαq)
      -SRF/RE-luc reporter assay (Gα12/13)
      -β-Arrestin assay
      -pERK assay

  GPCR Panel 筛选:

      -500+ cell lines
      -Full human, mouse, rat GPCR in panel
      -Agonist, antagonist, inverse agonist modes
      -Safety panel screening

   稳转细胞系构建:

     -Full human, mouse, rat GPCR in panel
     -GPCR overexpress /inducible cell lines
     -Cell line stability up to 20 passages
     -No promiscus G protein co-transfection
     -GPCR reporter gene cell lines(CRE-luc, NFAT-luc, SRF/RE-luc)
技术文档
HEK293 Pig GLP-1.pdf
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