How to ensure the purity and activity of the product?

We utilize advanced quality control processes, including high-performance liquid chromatography (HPLC), nuclear magnetic resonance (NMR), liquid chromatography-mass spectrometry (LC-MS), and other assays, to ensure that the purity and activity of our products meet the highest standards.

Can this compound library be used for cell-based functional screening experiments?

Absolutely. This compound library is optimized for cell-based drug screening. Compounds are dissolved in high-purity solvents such as DMSO and pre-validated to ensure low cytotoxicity. It can be directly applied to various functional assays, significantly streamlining experimental preparation.

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GPCR/G Protein-Targeted Compounds

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GPCR/G Protein-Targeted Compounds Applications Advantages Publication FAQs

Overview

(Source: Bioicons, free)

G protein-coupled receptors (GPCRs) are the largest and most diverse group of membrane receptors in eukaryotes. They act as "inboxes" for information on the cell surface, sensing information in the form of light energy, peptides, lipids, sugars, and proteins, and regulating cellular responses to environmental stimuli. There are nearly 1,000 different GPCRs in the human body, which are involved in almost all life activities and are essential for maintaining life and health. Therefore, GPCRs have become one of the most important drug targets, playing a key role in the discovery and development of drugs for major diseases, including cardiovascular diseases, metabolic diseases, neurological diseases, immune diseases, and cancer.

In exploring the complex mechanisms of obesity and metabolic diseases, precise research tools are the key to unlocking the unknown. As a leading provider of biological research products, Protheragen provides a series of GPCR/G protein-related products, which are designed to help clients unravel the mysteries of obesity and metabolic diseases and promote the development of related research.

Features of GPCR/G Protein

GPCR Signaling Pathways in Metabolism

Our company offers a diverse product line of GPCR agonists, antagonists, inhibitors, and other products to meet your needs in obesity and metabolic disease research. These products are used to study key aspects of GPCR signaling pathways, G protein-dependent and non-dependent mechanisms.

The extracellular region of GPCR undergoes conformational changes upon the binding of agonistic signaling molecules and regulates physiological activities in vivo through the cyclic adenosine monophosphate (cAMP) signaling pathway, the phosphatidylinositol signaling pathway, and the calcium ion signaling pathway.

Fig.1 Expression and function of various GPCRs in metabolic tissues. Fig.1 The expression and function of GPCRs in different metabolic tissues. (Oliveira de Souza, et al., 2021)

Precise Targeting

Our GPCR/G protein-related products are precisely targeted and act specifically on target receptors or proteins to achieve precise regulation of signal transduction pathways. This helps clients gain a deeper understanding of the mechanism of GPCR action in obesity and metabolic diseases and identify potential therapeutic targets.

Our products are closely related to the following receptors, so if you are looking for a specific product receptor, we are the best partner for you on your research pathway.

5-HT Receptor	5-HT Transporter	Adenosine receptor
Adrenergic receptor	Androgen receptor	Angiotensin II receptor
Aryl hydrocarbon receptor	B1 receptor	Bcl-2 Family
Beta-nerve growth factor	Bradykinin receptor	Dopamine transporter
Endothelin receptor	Glucagon receptor	Glucocorticoid receptor
H1 receptor	H2 receptor	H3 receptor
H4 receptor	Histamine receptor	Human glucagon receptor
IL receptor	Leukotriene receptor	NMDA receptor
NS4BH1 histamine receptor	Prostaglandin receptor	Rat glucagon receptor
Serotonin transporter	Serotonin transporter	TGF-β receptor
TNF receptor	α1A-adrenergic receptor	α1β1γ2 GABAA receptor
α1β2 GABAA receptor	α1β2γ2 GABAA receptor	α1β3γ2 GABAA receptor
α2-Adrenergic receptor	β1-Adrenergic receptor	β-Adrenergic receptor
δ-Opioid receptor	κ-Opioid receptor	μ-Opioid receptor

Applications

Obesity Research: Our products can be used to study the molecular mechanism of obesity occurrence and find potential therapeutic targets by regulating the GPCR/G protein signaling pathway.
Metabolic Disease Research: Our products can explore the role of GPCR/G proteins in metabolic diseases such as diabetes and hyperlipidemia, providing new ideas for disease treatment.
Drug R&D: Our products can be used for drug screening of GPCR/G proteins, accelerating the process of new drug development and improving the effectiveness and safety of drugs.

Advantages

Comprehensive Target Coverage

Our products cover a number of important targets of the GPCR family, which are clinically important in the areas of neurological and cardiovascular diseases, cancer, and metabolic diseases.

Extensive Compound Library

Our product library contains more than 2,500 molecular compounds with favorable biological and pharmacological activities, which provide strong support for your studies.

High Purity and Stability

Our products are subject to strict quality control to ensure high purity and stability. We offer GPCR/G protein compounds in pre-solution or solid form, which are dissolved according to the clients' requirements.

Publication

Title: Metabolic functions of G protein-coupled receptors and β-arrestin-mediated signaling pathways in the pathophysiology of type 2 diabetes and obesity

Journal: Frontiers in Endocrinology, 2021

DOI: https://doi.org/10.3389/fendo.2021.715877

Summary: This article reviews the importance of GPCRs and their signaling pathways, including G protein-dependent and β-inhibitory protein-dependent pathways, in the pathogenesis and treatment of metabolic diseases. GPCRs are involved in type 2 diabetes (T2D) pathogenesis by affecting insulin resistance and β-cell dysfunction, and their signaling pathways may serve as a therapeutic target to enhance insulin sensitivity. In addition, β-inhibitory proteins, as key regulators of GPCR signaling, coordinate complex signaling networks that specifically control metabolic homeostasis.

Fig.2 The concept of GPCR signaling: biased signaling. Fig.2 GPCRs and their signaling pathways. (Oliveira de Souza, et al., 2021)

Customer Review

Exceptional Target Hit Rate
"Protheragen's GPCR library is highly focused on metabolism-related receptors, ensuring our discovered hit compounds exhibit significantly higher quantities and specificity compared to other general compound libraries we've used. This specialized design substantially reduces our screening false positive rate."— Dr. L* H***

Precision Research on Biased Signaling
"This GPCR library contains a large number of compounds with biased agonist potential, which is crucial for optimizing the side effects of G protein agonists."— Prof. A* M***

Frequently Asked Questions

What are the research methods and advantages of GPCR activation mechanisms?

Tab.1 Research methods and advantages of GPCR activation mechanism. (Protheragen)

Method	Range	Advantages
Bioluminescence resonance energy transfer/Double electron-electron resonance	Single	Dynamic properties of receptors
Molecular dynamics simulation	Single	Atomic-level conformational changes
Nuclear magnetic resonance	Single	Fine local conformational changes
Residue contact scoring	Family	Fast and accurate
Single-particle cryo-electron microscopy	Single	Fast, near-atomic scale
X-ray	Single	Highly accurate 3D structures

How to ensure the purity and activity of the product?

We utilize advanced quality control processes, including high-performance liquid chromatography (HPLC), nuclear magnetic resonance (NMR), liquid chromatography-mass spectrometry (LC-MS), and other assays, to ensure that the purity and activity of our products meet the highest standards.
Can this compound library be used for cell-based functional screening experiments?

Absolutely. This compound library is optimized for cell-based drug screening. Compounds are dissolved in high-purity solvents such as DMSO and pre-validated to ensure low cytotoxicity. It can be directly applied to various functional assays, significantly streamlining experimental preparation.

The GPCR/G protein products provided by Protheragen not only have significant advantages in terms of technology and services but also demonstrate excellent capabilities in meeting clients' needs and accelerating drug discovery. If you are interested in our products, please feel free to contact us!

Reference

Oliveira de Souza, C.; et al. Metabolic functions of G protein-coupled receptors and β-arrestin-mediated signaling pathways in the pathophysiology of type 2 diabetes and obesity. Frontiers in Endocrinology. 2021, 12: 715877. (CC BY 4.0)