WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H531847
CAS#: 1391076-61-1
Description: GLPG0974 is a potent and selective FFA2 antagonist.
Hodoodo Cat#: H531847
Name: GLPG0974
CAS#: 1391076-61-1
Chemical Formula: C25H25ClN2O4S
Exact Mass: 484.12
Molecular Weight: 484.990
Elemental Analysis: C, 61.91; H, 5.20; Cl, 7.31; N, 5.78; O, 13.20; S, 6.61
Related CAS #: 1391076-61-1
Synonym: GLPG0974; GLPG 0974; GLPG-0974.
IUPAC/Chemical Name: 4-[[(2R)-1-(1-benzothiophene-3-carbonyl)-2-methylazetidine-2-carbonyl]-[(3-chlorophenyl)methyl]amino]butanoic acid
InChi Key: MPMKMQHJHDHPBE-RUZDIDTESA-N
InChi Code: 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
SMILES Code: O=C(O)CCCN(C([C@]1(C)N(C(C2=CSC3=CC=CC=C23)=O)CC1)=O)CC4=CC=CC(Cl)=C4
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info:
Biological target: | |
In vitro activity: | |
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The following data is based on the product molecular weight 484.99 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
Formulation protocol: | |
In vitro protocol: | |
In vivo protocol: |
1: Namour F, Galien R, Van Kaem T, Van der Aa A, Vanhoutte F, Beetens J, Van't Klooster G. Safety, pharmacokinetics and pharmacodynamics of GLPG0974, a potent and selective FFA2 antagonist, in healthy male subjects. Br J Clin Pharmacol. 2016 Jul;82(1):139-48. doi: 10.1111/bcp.12900. PubMed PMID: 26852904; PubMed Central PMCID: PMC4917808.
2: Sergeev E, Hansen AH, Pandey SK, MacKenzie AE, Hudson BD, Ulven T, Milligan G. Non-equivalence of Key Positively Charged Residues of the Free Fatty Acid 2 Receptor in the Recognition and Function of Agonist Versus Antagonist Ligands. J Biol Chem. 2016 Jan 1;291(1):303-17. doi: 10.1074/jbc.M115.687939. PubMed PMID: 26518871; PubMed Central PMCID: PMC4697166.
3: Pizzonero M, Dupont S, Babel M, Beaumont S, Bienvenu N, Blanqué R, Cherel L, Christophe T, Crescenzi B, De Lemos E, Delerive P, Deprez P, De Vos S, Djata F, Fletcher S, Kopiejewski S, L'Ebraly C, Lefrançois JM, Lavazais S, Manioc M, Nelles L, Oste L, Polancec D, Quénéhen V, Soulas F, Triballeau N, van der Aar EM, Vandeghinste N, Wakselman E, Brys R, Saniere L. Discovery and optimization of an azetidine chemical series as a free fatty acid receptor 2 (FFA2) antagonist: from hit to clinic. J Med Chem. 2014 Dec 11;57(23):10044-57. doi: 10.1021/jm5012885. PubMed PMID: 25380412.