MedKoo Cat#: 531847 | Name: GLPG0974
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

GLPG0974 is a selective GPR43 (FFAR2) antagonist developed to modulate short-chain fatty acid (SCFA) signaling in inflammatory diseases. It inhibits neutrophil chemotaxis and pro-inflammatory cytokine release, demonstrating potential in treating inflammatory bowel disease (IBD). Preclinical studies show nanomolar potency (IC₅₀ ~10–100 nM), reducing gut inflammation by blocking SCFA-induced immune activation.

Chemical Structure

GLPG0974
GLPG0974
CAS#1391076-61-1

Theoretical Analysis

MedKoo Cat#: 531847

Name: GLPG0974

CAS#: 1391076-61-1

Chemical Formula: C25H25ClN2O4S

Exact Mass: 484.1224

Molecular Weight: 484.99

Elemental Analysis: C, 61.91; H, 5.20; Cl, 7.31; N, 5.78; O, 13.20; S, 6.61

Price and Availability

Size Price Availability Quantity
25mg USD 850.00 2 Weeks
50mg USD 1,350.00 2 Weeks
100mg USD 2,350.00 2 Weeks
200mg USD 3,950.00 2 Weeks
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Related CAS #
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

Preparing Stock Solutions

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.

Recalculate based on batch purity %
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
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.