| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
The (S)-enantiomer itself is a non-active isomer that does not effectively bind to or block the free fatty acid receptor-2 (FFA2/GPR43). In contrast, GLPG0974 acts as a specific antagonist of FFA2/GPR43, a G-protein-coupled receptor involved in immune responses and metabolic regulation.
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|---|---|
| ln Vitro |
(S)-GLPG0974 is used as an inactive control, so it has minimal activity in vitro. It may show some weak binding to FFA2 but lacks functional antagonist activity. It is used to demonstrate the stereoselectivity of FFA2 inhibition and to control for off-target effects of GLPG0974.
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| ln Vivo |
In vivo, (S)-GLPG0974 is used as a negative control to compare with the active isomer. It should not produce the pharmacological effects (e.g., inhibition of FFA2-mediated signaling) seen with GLPG0974. Its value lies in establishing that observed in vivo effects are specifically due to FFA2 antagonism.
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| Enzyme Assay |
(S)-GLPG0974 is not used as an active compound in enzyme/receptor binding assays; it is a control. Typical protocols for its active counterpart GLPG0974 involve radioligand binding assays using membranes from cells expressing recombinant human FFA2. (S)-GLPG0974 (0.1 nM-10 uM) is tested in parallel to demonstrate selectivity.
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| Cell Assay |
For cell-based assays, (S)-GLPG0974 is used as a negative control. Typical protocols involve treating FFA2-expressing cells (e.g., neutrophils) with GLPG0974 or (S)-GLPG0974 (1-100 nM) prior to stimulation with FFA2 agonists (e.g., propionate). FFA2 activation is measured by calcium flux, ERK phosphorylation, or beta-arrestin recruitment.
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| Animal Protocol |
In vivo, (S)-GLPG0974 is used as a control in animal models. Typical protocols involve administering (S)-GLPG0974 or GLPG0974 (0.1-10 mg/kg, oral or intraperitoneal) to mice prior to FFA2 agonist challenge or in disease models (e.g., colitis, asthma). The inactive isomer should not provide therapeutic benefit.
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| ADME/Pharmacokinetics |
No pharmacokinetic data specifically for (S)-GLPG0974 is available. As a single enantiomer with the same molecular formula (C25H25ClN2O4S, MW 485.00) as GLPG0974, it is expected to have similar PK properties but without the pharmacodynamic effects. Detailed studies would be needed for confirmation.
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| Toxicity/Toxicokinetics |
No direct toxicity data is available for (S)-GLPG0974. As an inactive control compound, it is not expected to cause significant toxicity at the concentrations used in experiments. However, standard laboratory safety precautions should be followed when handling this research chemical.
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| References | |
| Additional Infomation |
(S)-GLPG0974 is a research-use compound that is not a pharmaceutical for human consumption. GLPG0974 is a free fatty acid receptor-2 antagonist that has been investigated for inflammatory and metabolic diseases but has not received regulatory approval. (S)-GLPG0974 is supplied as a powder with purity ≥95% and is typically stored at -20degC for up to 3 years.
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| Exact Mass |
484.122
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|---|---|
| CAS # |
2326220-69-1
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| Related CAS # |
GLPG0974;1391076-61-1
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| PubChem CID |
89894283
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
33
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| Complexity |
752
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| Defined Atom Stereocenter Count |
1
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| SMILES |
C[C@]1(CCN1C(=O)C2=CSC3=CC=CC=C32)C(=O)N(CCCC(=O)O)CC4=CC(=CC=C4)Cl
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| InChi Key |
MPMKMQHJHDHPBE-VWLOTQADSA-N
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| 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-/m0/s1
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| Chemical Name |
4-[[(2S)-1-(1-benzothiophene-3-carbonyl)-2-methylazetidine-2-carbonyl]-[(3-chlorophenyl)methyl]amino]butanoic acid
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~105 mg/mL (~216.5 mM; with ultrasonication)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 5.25 mg/mL (10.82 mM) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), Suspended solution; with ultrasonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (52.5 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 5.25 mg/mL (10.82 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), Clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (52.5 mg/mL) to 900 μL of corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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