GPCR Research Reagents and Assays

G蛋白偶联受体（GPCR）是结构变化多样的一大类蛋白膜受体，包括：β1和β2肾上腺素能受体、多巴胺能受体和胆碱能受体。我们可提供G蛋白偶联受体研究所需的所有先进检测分析设备。

以及多种靶标Gs-、Gq-和Gi-偶联受体的实验试剂。我们产品还包括：

荧光、发光或吸收光检测所需的可调焦GPCR细胞成像仪和液体工作站；
经优化的GPCR细胞水平检测平台
多样检测试剂——GPCR稳定表达细胞系、冷冻即用型GPCR细胞株及细胞膜制品，以及放射性配体等
我们完备的产品组合能够满足GPCR研究的全部需求。您可借助以上仪器及试剂产品进行如下GPCR的研究应用：
GPCR通路激活研究：细胞内钙流、cAMP、磷酸化ERK，肌醇磷脂IP变化等
GPCR信号通路报告基因试验
受体配体结合
GTP-γ-S结合活性

Ligand Binding

The ligand/receptor binding is the first key step in GPCR signaling. PerkinElmer offers a range of ligand/receptor interaction solutions in both radioactive format and fluorescence assays with our proprietary HTRF-based Tag-lite technology.

Tag-lite^® - Tag-lite is a non-radioactive TR-FRET-based solution which can be used to assess the pharmacology and pharmacodynamics of ligand/receptor interactions. The receptor of interest is labeled with cryptate in a way that does not alter receptor binding. The corresponding ligand is labeled with d2 acceptor. When the d2-labeled ligand binds to the cryptate-labeled receptor, it produces a HTRF signal.

In a competition assay, the introduction of a competing small molecule dislodges the d2-labeled ligand. Consequently, the ligand is pushed away and the signal stops.

Tag-lite principle
Receptor ligand binding with radiolabeled ligands and GPCR membranes - We also offer a range of radioactive ligands, which are used to study molecular interactions and QC our GPCR over-expressing cell lines and membrane preparations. Radiometric ligand binding assays are conducted on cells or cell membranes containing a GPCR receptor of interest. Radioligands can be used to perform saturation curves, competition, and kinetic experiments.

Radiometric ligand-binding assays

Radioactive ligand binding assays can be performed in several different formats. Typically, we perform this assay in filtration format, where the unbound ligand is washed away using a vacuum manifold or cell harvester. The assay can also be conducted in a homogenous Scintillation Proximity Assay (SPA) format, where no wash steps are required.

Over 100 GPCR-expressing membrane preparations are validated for receptor ligand binding and over 50 are validated for GTPγS binding.

建议内容

See our full selection of SPA assay reagents here See our full selection of GPCR membranes here See our full selection of iodinated compounds Discover our full selection of radiolabeled ligands More information on radiometric ligand-binding assays Determination of association and dissociate rates application note

G-protein Activation

The main signal transduction of GPCRs is dependent on the receptor-mediated activation of heterotrimeric G-proteins.

G-proteins are composed of three subunits (Gα, Gβ and Gγ) and are classified into four families (Gs, Gi/o, Gq/11, and G12/13):

Gαs-coupled GPCRs positively stimulate the activity of adenylate cyclase, resulting in an increase in cellular cAMP
Gαi-coupled GPCRs lead to a negative regulation of adenylate cyclase, and thus to a decrease in cAMP production
Gαq protein signaling is based on enzymes of the phospholipase C family (PLC).

GPCR/G-protein signaling pathways

建议内容

HTRF GTP Gi binding assay HTRF IP-one Gq kit HTRF cAMP Gs Dynamic kit HTRF cAMP Gi kit Find out about our GTP Binding portfolio: radioactive GTPγS assay

Arrestins Recruitment

GPCRs also initiate G-protein-independent pathways that instead rely on arrestin coupling, which in turn suppresses G-protein activation.

When a ligand binds to the extracellular part of a GPCR, the receptor undergoes conformational changes and opens its intracellular part to be phosphorylated by kinases. This phosphorylation of GPCRs by GRKs (GPCR kinases) is a prerequisite for high-affinity arrestin binding. The phosphorylated GPCR becomes a binding site for arrestins. Once linked, arrestins can interact with several partners such as AP2 or signaling proteins.

Arrestin signaling pathways

建议内容

AP2 total kit β-arrestin 2 total kit β-arrestin 1 total kit β-arr2 recruitment kit to monitor endogenous β-arrestin 2 recruitment mediated by GPCR activation Deepen your β-Arrestin Knowledge White Paper

Intracellular Signaling

GPCRs are at the beginning of many phosphorylation cascades involving phosphatases bound to second messengers.

Following the activation of a GPCR, signals are sent via G-proteins and arrestins to second messengers. Each GPCR has its own signaling pathway, but kinases and phosphatases are always involved and promote phosphorylation cascades to the nucleus. These molecular events are implicated in many physiological and cellular processes such as cell survival, proliferation, differentiation, and metabolism.

Intracellular signaling pathway

建议内容

HTRF phospho-proteins kits Key guidelines to successful cell signaling experiments guide See Alpha Surefire kits

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1-25 的 257 产品与服务

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GTP Gi binding assay, 500 Tests

62GTPPEG

The GTP Gi binding assay is designed to quantify GTP recruitment by activated Gi protein in membrane-bound GPCR models.
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Vasopressin/Oxytocin V2R fluorescent probe, 1 Item

L0063RED

This Vasopressin receptor red antagonist is a Vasopressin V2 Benzazepine derivative labeled with a red emitting HTRF fluorescent probe.
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Stimulation Buffer 2 (5X), 8 ml

62IP1FDC

Stimulation Buffer 2 is spare part intended for use in the IP-One Gq kits
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Stimulation Buffer 2 (5X), 100 ml

62IP1FDG

Stimulation Buffer 2 is spare part intended for use in the IP-One Gq kits
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Stimulation Buffer 1 (5X), 8 ml

64SB1FDC

Stimulation Buffer 1 is spare part intended for use in the cAMP Gs dynamic, cAMP Gs HiRange and cAMP Gi kits
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Stimulation Buffer 1 (5X), 100 ml

64SB1FDD

Stimulation Buffer 1 is spare part intended for use in the cAMP Gs dynamic, cAMP Gs HiRange and cAMP Gi kits
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SNAP-Red labeling reagent, 100 nmol

SSNPREDF

SNAP-Tag, Clip-Tag, and HALO-Tag are protein labeling systems enabling the covalent attachement of fluorophores onto proteins of interest. SNAP-Red enables SNAP-tagged proteins to become labeled with a red fluorophore.
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SNAP-Red labeling reagent, 500 nmol

SSNPREDZ

SNAP-Tag, Clip-Tag, and HALO-Tag are protein labeling systems enabling the covalent attachement of fluorophores onto proteins of interest. SNAP-Red enables SNAP-tagged proteins to become labeled with a red fluorophore.
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SNAP-Red labeling reagent, 20 nmol

SSNPREDE

SNAP-Tag, Clip-Tag, and HALO-Tag are protein labeling systems enabling the covalent attachement of fluorophores onto proteins of interest. SNAP-Red enables SNAP-tagged proteins to become labeled with a red fluorophore.
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SNAP-Lumi4-Tb labeling reagent, 25 nmol

SSNPTBG

SNAP-Tag, Clip-Tag, and HALO-Tag are protein labeling systems enabling the covalent attachement of fluorophores onto proteins of interest. SNAP-Lumi4-Tb enables SNAP-tagged proteins to become labeled with a Terbium fluorophore.
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SNAP-Lumi4-Tb labeling reagent, 5 nmol

SSNPTBD

SNAP-Tag, Clip-Tag, and HALO-Tag are protein labeling systems enabling the covalent attachement of fluorophores onto proteins of interest. SNAP-Lumi4-Tb enables SNAP-tagged proteins to become labeled with a Terbium fluorophore.
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SNAP-Lumi4-Tb labeling reagent, 2 nmol

SSNPTBC

SNAP-Tag, Clip-Tag, and HALO-Tag are protein labeling systems enabling the covalent attachement of fluorophores onto proteins of interest. SNAP-Lumi4-Tb enables SNAP-tagged proteins to become labeled with a Terbium fluorophore.
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SNAP-Lumi4-Tb labeling reagent, 100 nmol

SSNPTBX

SNAP-Tag, Clip-Tag, and HALO-Tag are protein labeling systems enabling the covalent attachement of fluorophores onto proteins of interest. SNAP-Lumi4-Tb enables SNAP-tagged proteins to become labeled with a Terbium fluorophore.
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SNAP-Green labeling reagent, 25 nmol

SSNPGRNF

SNAP-Tag, Clip-Tag, and HALO-Tag are protein labeling systems enabling the covalent attachement of fluorophores onto proteins of interest. SNAP-Green enables SNAP-tagged proteins to become labeled with a green fluorophore.
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SNAP-Green labeling reagent, 5 nmol

SSNPGRNE

SNAP-Tag, Clip-Tag, and HALO-Tag are protein labeling systems enabling the covalent attachement of fluorophores onto proteins of interest. SNAP-Green enables SNAP-tagged proteins to become labeled with a green fluorophore.
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SNAP-Green labeling reagent, 100 nmol

SSNPGRNZ

SNAP-Tag, Clip-Tag, and HALO-Tag are protein labeling systems enabling the covalent attachement of fluorophores onto proteins of interest. SNAP-Green enables SNAP-tagged proteins to become labeled with a green fluorophore.
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Tag-lite Buffer (5X), 100 ml

LABMED

The Tag-lite buffer is a labeling buffer to be used as part of the Tag-lite labeling protocol.
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Tag-lite T8-SNAP (Zeocin) plasmid, 10 ml

PT8SNAPZEO

Tag-lite plasmid featuring a SNAP-Tag sequence, a T8 peptide sequence, and a Zeocin resistance gene.Cloning and expression of the GPCR of interest as a SNAP-Tag or CLIP-Tag fusion protein enables its subsequent labeling with Terbium.
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Tag-lite T8-SNAP (Neomycin) plasmid, 10 ml

PT8SNAPNEO

Tag-lite plasmid featuring a SNAP-Tag sequence, a T8 peptide sequence, and a Neomycin resistance gene.Cloning and expression of the GPCR of interest as a SNAP-Tag or CLIP-Tag fusion protein enables its subsequent labeling with Terbium.
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Tag-lite T8-SNAP (Hygromycin) plasmid, 10 mg

PT8SNAPHYG

Tag-lite plasmid featuring a SNAP-Tag sequence, a T8 peptide sequence, and a Hygromycin resistance gene.Cloning and expression of the GPCR of interest as a SNAP-Tag or CLIP-Tag fusion protein enables its subsequent labeling with Terbium.
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Tag-lite T8-HaloTag (Zeocin) plasmid, 10 mg

PT8HALOZEO

Tag-lite plasmid featuring a HALO-Tag sequence, a T8 peptide sequence, and a Zeocin resistance gene.Cloning and expression of the GPCR of interest as a SNAP-Tag or CLIP-Tag fusion protein enables its subsequent labeling with Terbium.
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Tag-lite T8-HaloTag (Neomycin) plasmid, 10 mg

PT8HALONEO

Tag-lite plasmid featuring a HALO-Tag sequence, a T8 peptide sequence, and a Neomycin resistance gene.Cloning and expression of the GPCR of interest as a SNAP-Tag or CLIP-Tag fusion protein enables its subsequent labeling with Terbium.
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Tag-lite T8-HaloTag (Hygromycin) plasmid, 10 mg

PT8HALOHYG

Tag-lite plasmid featuring a HALO-Tag sequence, a T8 peptide sequence, and a Hygromycin resistance gene.Cloning and expression of the GPCR of interest as a SNAP-Tag or CLIP-Tag fusion protein enables its subsequent labeling with Terbium.
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Tag-lite T8-CLIP (Zeocin) plasmid, 10 mg

PT8CLIPZEO

Tag-lite plasmid featuring a CLIP-Tag sequence, a T8 peptide sequence, and a Zeocin resistance gene.Cloning and expression of the GPCR of interest as a SNAP-Tag or CLIP-Tag fusion protein enables its subsequent labeling with Terbium.
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Tag-lite T8-CLIP (Neomycin) plasmid, 10 Item

PT8CLIPNEO

Tag-lite plasmid featuring a CLIP-Tag sequence, a T8 peptide sequence, and a Neomycin resistance gene.Cloning and expression of the GPCR of interest as a SNAP-Tag or CLIP-Tag fusion protein enables its subsequent labeling with Terbium.