Search by product name, CAS, target or catalog number. Press Down Arrow to reach product suggestions, Tab to move between links, and Escape to close suggestions.
GPR agonists and antagonists act on numbered G protein-coupled receptors (GPRs), many first described as orphans. Several of these receptors sense nutrients and metabolites, which links them to glucose and lipid metabolism research. GPR40, also called free fatty acid receptor 1 (FFAR1), was shown in 2003 to be activated by medium- and long-chain fatty acids. On pancreatic beta cells, GPR40 mediates fatty acid enhancement of glucose-stimulated insulin secretion. GPR119 was deorphanized in 2006 as a receptor for the lipid amide oleoylethanolamide. Fasiglifam is a GPR40 agonist and MBX-2982 a GPR119 agonist. TC-G-1008 activates the zinc-sensing receptor GPR39, and MK-6892 is an agonist of GPR109A.
GSK682753A is a selective and highly potent inverse agonist of the epstein-barr virus-induced receptor 2 (EBI2) with an IC50 of 53.6 nM.
AF64394 is a GPR3 inverse agonist, with a pIC50 of 7.3.
GPR183 inverse agonist-1 is a potent inverse agonist targeting the G protein-coupled receptor GPR183. It effectively inhibits GPR183-mediated Gi activation and prevents β-arrestin2 recruitment, thereby blocking the migration of peripheral blood mononuclear cells (PBMCs). This compound is valuable for research into inflammatory, autoimmune, and neoplastic disorders, enabling scientists to explore its therapeutic potential in these fields.
Out of stock
All 3 sizes
BTI-A-404 is a selective and competitive inverse agonist of the human G protein-coupled receptor GPR43. This compound exhibits potent inhibitory activity, making it valuable for studying mechanisms related to inflammation, obesity, and type 2 diabetes. BTI-A-404 aids in elucidating the role of GPR43 in metabolic disorders and inflammatory responses, providing essential insights for therapeutic development.
Synonyms: CVN424
Solangepras is a selective inverse agonist of GPR6, exhibiting a Ki of 9.4 nM and an EC50 of 38 nM. This compound is capable of penetrating the blood-brain barrier, making it a valuable tool for investigating the role of GPR6 in neurological conditions. Solangepras holds potential for advancing research in Parkinson's disease and related disorders.
GPR6 inverse agonist 2 is a selective inverse agonist targeting the GPR6 receptor, exhibiting an IC50 of less than 0.1 μM. This compound shows notable selectivity over GPR3, with IC50 values ranging from 1 to 30 μM, and demonstrates preliminary cardiac safety with an IC50 of 21.71 μM for hERG. GPR6 inverse agonist 2 is suitable for research applications investigating movement disorders, including Parkinson's disease, offering valuable insights into therapeutic avenues for these conditions.
Out of stock
All 3 sizes
GPR6 inverse agonist 1 is a selective inverse agonist for the GPR6 receptor, demonstrating an IC50 of less than 100 nM. This compound is essential for research investigating the pathological mechanisms of neurodegenerative disorders, particularly Parkinson's disease and Huntington's disease. Its ability to modulate GPR6 activity makes it a valuable tool for studying these conditions and exploring potential therapeutic strategies.
Out of stock
All 3 sizes