GLPG0974

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GLPG0974

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Cat No: 28108

Biochemicals - Receptor Pharmacology

GLPG0974 is an antagonist of free fatty acid receptor 2 (FFAR2/GPR43; IC50 = 9 nM).{46506} It is selective for FFAR2 over FFAR3 at concentrations up to 30 μM and over a panel of 55 receptors, ion channels, and transporters at 10 μM. GLPG0974 inhibits ...

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Territorial Availability: Available through Bertin Technologies only in France

Synonyms:

4-[[[(2R)-1-(benzo[b]thien-3-ylcarbonyl)-2-methyl-2-azetidinyl]carbonyl][(3-chlorophenyl)methyl]amino]-butanoic acid

Correlated keywords:

GLPG-0974 FA FFAR-2 3 GPR-43 CD-11b CD11-b hFFAR2DREADD GLP1

Product Overview:
GLPG0974 is an antagonist of free fatty acid receptor 2 (FFAR2/GPR43; IC50 = 9 nM).{46506} It is selective for FFAR2 over FFAR3 at concentrations up to 30 μM and over a panel of 55 receptors, ion channels, and transporters at 10 μM. GLPG0974 inhibits acetate-induced migration of isolated human neutrophils in buffer or plasma (IC50s = 27 and 43 nM, respectively), as well as acetate-induced expression of CD11b activation-specific epitope on neutrophils in isolated human whole blood (IC50 = 438 nM). GLPG0974 also inhibits a human FFAR2-based designer receptor exclusively activated by designer drugs (hFFAR2-DREADD; IC50 = 36.31 nM in a cell-based β-arrestin-2 recruitment assay).{46507} It inhibits glucagon-like peptide 1 (GLP-1) secretion induced by the hFFA2-DREADD ligand sorbic acid in isolated colonic crypts from mice expressing hemagglutinin-tagged hFFAR2-DREADD when used at a concentration of 10 μM.

Size	1 mg
Shipping	dry ice
CAS Number	1391076-61-1
Molecular Formula	C₂₅H₂₅ClN₂O₄S
SMILES	O=C(N1CC[C@]1(C)C(N(CC2=CC(Cl)=CC=C2)CCCC(O)=O)=O)C3=CSC4=C3C=CC=C4
Molecular Weight	485
Formulation	A solid
Purity	≥98%
Custom Code	2903.99
UNSPSC code	12352100

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Cayman Chemical's mission is to help make research possible by supplying scientists worldwide with the basic research tools necessary for advancing human and animal health. Our utmost commitment to healthcare researchers is to offer the highest quality products with an affordable pricing policy.

Our scientists are experts in the synthesis, purification, and characterization of biochemicals ranging from small drug-like heterocycles to complex biolipids, fatty acids, and many others. We are also highly skilled in all aspects of assay and antibody development, protein expression, crystallization, and structure determination.

Over the past thirty years, Cayman developed a deep knowledge base in lipid biochemistry, including research involving the arachidonic acid cascade, inositol phosphates, and cannabinoids. This knowledge enabled the production of reagents of exceptional quality for cancer, oxidative injury, epigenetics, neuroscience, inflammation, metabolism, and many additional lines of research.

Our organic and analytical chemists specialize in the rapid development of manufacturing processes and analytical methods to carry out clinical and commercial GMP-API production. Pre-clinical drug discovery efforts are currently underway in the areas of bone restoration and repair, muscular dystrophy, oncology, and inflammation. A separate group of Ph.D.-level scientists are dedicated to offering Hit-to-Lead Discovery and Profiling Services for epigenetic targets. Our knowledgeable chemists can be contracted to perform complete sample analysis for analytes measured by the majority of our assays. We also offer a wide range of analytical services using LC-MS/MS, HPLC, GC, and many other techniques.

Accreditations
ISO/IEC 17025:2005
ISO Guide 34:2009

Cayman is a leader in the field of emerging drugs of abuse, providing high-purity Schedule I-V Controlled Substances to federally-licensed laboratories and qualified academic research institutions for forensic analyses. We are certified by ACLASS Accreditation Services with dual accreditation to ISO/IEC 17025:2005 and ISO Guide 34:2009.