GPCR Profiling Services with Various Panels

Creative Biolabs is the specialist provider of GPCR Profiling Services with Various Panels. Our team of dedicated scientists will provide customers with the comprehensive and rapid safety evaluation of lead compounds through standard experimental procedures to meet their GPCR drug discovery needs. The GPCR profiling services include:

Indispensable Drug Safety Evaluation Panel in GPCR Drug Development Process

G protein-coupled receptors (GPCRs) are one of the most prominent drug targets in current research. However, the failure of the lead compound due to safety issues remains an obstacle to bringing GPCR drugs to market. This is because the lead compound may interact with other unexpected therapeutic targets of GPCR, leading to possible side effects or even life-threatening effects. GPCR Profiling Services with Various Panels can be used in vitro to evaluate the safety of lead compounds by functional activity screening method to stimulate or inhibit the targeted GPCR. It provides a reference for the later study of lead compounds.

Creative Biolabs can set agonist and antagonist modes as well as single or multiple tests to detect Ca²⁺ flow response curves using the Fluorescent Imaging Plate Reader (FLIPR) for high-throughput analysis of compounds. Safety panel detection of lead compounds is beneficial to evaluate the safety of compounds in the early stage and avoid some serious adverse reactions in the later stage, thus saving more costs and time.

Fig.1. Novel fluorescence-based high-throughput FLIPR assay utilizing membrane-tethered genetic calcium sensors to identify T-type calcium channel modulators.¹

Fig.2. EC50 values of 2-iodomelatonin were 19.4 nM and 13.8 nM measured in the FLIPR calcium assay in the single assay format (FLIPR) and multiplexed assay format (Multip), respectively.²

Our Feature Service

• All you need to do is provide the compound and explain the method of processing, solubility, and storage.
• High throughput. Large numbers of GPCRs and compounds can be screened at one time.
• Reduce the time and cost of later validation of compounds in vivo.
• Predicting possible adverse side effects of lead compounds in clinical trials in vivo.
• High data accuracy. Adoption of functional activity screening.

With years of experience in safety pharmacology in vitro, Creative Biolabs can provide a wide range of target GPCRs that have been validated by researchers and the pharmaceutical industry for important safety evaluations, enabling you to select the best drug candidates in a short time to bring drugs to market as quickly as possible. Please contact us to discuss your project and we will tailor your high-throughput GPCR Profiling Services with Various Panels package to meet your goals.

References

1. Zhang, Y. L.; et al. Novel fluorescence-based high-throughput FLIPR assay utilizing membrane-tethered genetic calcium sensors to identify T-type calcium channel modulators. ACS Pharmacology & Translational Science. 2022; 5(3):156-168.
2. Sheth, H.; et al. A multiplexed fluorescent calcium and NFAT Reporter gene assay to identify GPCR agonists. Current chemical genomics and translational medicine. 2013; 7:1-8.