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GLPG 0974 - ≥98%(HPLC), high purity , CAS No.1391076-61-1, Antagonist of FFA2 receptor

  • Moligand™
  • ≥98%(HPLC)
Item Number
G287679
Grouped product items
SKUSizeAvailabilityPrice Qty
G287679-1mg
1mg
In stock
$33.90
G287679-5mg
5mg
In stock
$139.90
G287679-10mg
10mg
In stock
$232.90
G287679-25mg
25mg
In stock
$484.90

Potent FFA2 (GPR43) antagonist

View related series
FFA2 receptor Antagonist

Basic Description

SynonymsGLPG0974|1391076-61-1|GLPG-0974|GLPG 0974|X7REK61AIS|4-[[(2R)-1-(1-benzothiophene-3-carbonyl)-2-methylazetidine-2-carbonyl]-[(3-chlorophenyl)methyl]amino]butanoic acid|CHEMBL3353541|4-[[[(2R)-1-(Benzo[b]thien-3-ylcarbonyl)-2-methyl-2-azetidinyl]carbonyl][
Specifications & Purity≥98%(HPLC)
Storage TempStore at -20°C
Shipped InIce chest + Ice pads
GradeMoligand™
Action TypeANTAGONIST
Mechanism of actionAntagonist of FFA2 receptor
Product Description

Product description

GLPG0974 is a free fatty acid receptor-2 (FFA2/GPR43) antagonist with an IC50 of 9 nM.

Associated Targets

FFAR2 Tchem Free fatty acid receptor 2 3 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

Names and Identifiers

IUPAC Name 4-[[(2R)-1-(1-benzothiophene-3-carbonyl)-2-methylazetidine-2-carbonyl]-[(3-chlorophenyl)methyl]amino]butanoic acid
INCHI InChI=1S/C25H25ClN2O4S/c1-25(11-13-28(25)23(31)20-16-33-21-9-3-2-8-19(20)21)24(32)27(12-5-10-22(29)30)15-17-6-4-7-18(26)14-17/h2-4,6-9,14,16H,5,10-13,15H2,1H3,(H,29,30)/t25-/m1/s1
InChi Key MPMKMQHJHDHPBE-RUZDIDTESA-N
Canonical SMILES CC1(CCN1C(=O)C2=CSC3=CC=CC=C32)C(=O)N(CCCC(=O)O)CC4=CC(=CC=C4)Cl
Isomeric SMILES C[C@@]1(CCN1C(=O)C2=CSC3=CC=CC=C32)C(=O)N(CCCC(=O)O)CC4=CC(=CC=C4)Cl
Alternate CAS 1391076-61-1
PubChem CID 57520598
MeSH Entry Terms 4-(((R)-1-(benzo(b)thiophene-3-carbonyl)-2-methyl-azetidine-2-carbonyl)-(3-chloro-benzyl)-amino)-butyric acid;GLPG0974
Molecular Weight 485

Certificates

Certificate of Analysis(COA)

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8 results found

Lot NumberCertificate TypeDateItem
F2302432Certificate of AnalysisApr 10, 2023 G287679
F2302433Certificate of AnalysisApr 10, 2023 G287679
F2302434Certificate of AnalysisApr 10, 2023 G287679
F2302436Certificate of AnalysisApr 10, 2023 G287679
F2302437Certificate of AnalysisApr 10, 2023 G287679
F2302438Certificate of AnalysisApr 10, 2023 G287679
F2302439Certificate of AnalysisApr 10, 2023 G287679
F2302442Certificate of AnalysisApr 10, 2023 G287679

Chemical and Physical Properties

SolubilitySolvent:DMSO, Max Conc. mg/mL: 48.5, Max Conc. mM: 100; Solvent:ethanol, Max Conc. mg/mL: 48.5, Max Conc. mM: 100

Related Documents

References

1. Pizzonero M, Dupont S, Babel M, Beaumont S, Bienvenu N, Blanqué R, Cherel L, Christophe T, Crescenzi B, De Lemos E et al..  (2014)  Discovery and optimization of an azetidine chemical series as a free fatty acid receptor 2 (FFA2) antagonist: from hit to clinic..  J Med Chem,  57  (23): (10044-57).  [PMID:25380412]
2. Namour F, Galien R, Van Kaem T, Van der Aa A, Vanhoutte F, Beetens J, Van't Klooster G.  (2016)  Safety, pharmacokinetics and pharmacodynamics of GLPG0974, a potent and selective FFA2 antagonist, in healthy male subjects..  Br J Clin Pharmacol,  82  (1): (139-48).  [PMID:26852904]

Solution Calculators