| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg | |||
| 100mg | |||
| Other Sizes |
| Targets |
GLPG0974 targets the free fatty acid receptor 2 (FFA2/GPR43). It is a potent and selective antagonist of this receptor. Its IC50 for FFA2 is 9 nM. By blocking FFA2, it inhibits short-chain fatty acid (SCFA)-induced neutrophil activation and migration.
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|---|---|
| ln Vitro |
In vitro, GLPG0974 significantly suppresses buffer salt-induced neutrophil migration. In a human whole blood assay, it also shows suppression of the neutrophil pharmacodynamic (PD) marker CD11b activating buffer epitope [AE][1].
In vitro, GLPG0974 is a potent antagonist of FFA2 with an IC50 of 9 nM. It inhibits acetate-induced neutrophil migration strongly in vitro with an IC50 of 27 nM. It also inhibits CD11b activation in a human whole blood assay. |
| ln Vivo |
GLPG0974 demonstrated exceptional pharmacokinetic characteristics concerning toxicity, with a 47% bioavailability and a dosage rise that was linear following 5 and 30 mg/kg of the powdered medication. The program's objective of achieving lengthy target coverage in people is congruent with the reported rise in half-life following higher doses of Manhattan [1].
In vivo, GLPG0974 has been shown to inhibit neutrophil-based pharmacodynamic markers. Its ability to inhibit neutrophil migration suggests potential for treating inflammatory diseases. Detailed in vivo efficacy data is not provided in the search results. |
| Enzyme Assay |
In vitro enzyme/receptor binding assays for GLPG0974 involve measuring its binding affinity to FFA2. These assays typically use radiolabeled ligands and membrane preparations from cells expressing the receptor. The IC50 value is determined from competition binding experiments.
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| Cell Assay |
In vitro cell-based assays for GLPG0974 involve treating neutrophils with the compound to assess its effects on migration and activation. Its ability to inhibit CD11b activation is measured using flow cytometry. Its effects on SCFA-induced signaling are also studied.
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| Animal Protocol |
In vivo animal experiments for GLPG0974 have not been detailed in the available sources. Its potential for treating inflammatory diseases is based on its in vitro activity.
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| ADME/Pharmacokinetics |
GLPG0974 has a molecular weight of 485.00 and a molecular formula of C25H25ClN2O4S. Specific pharmacokinetic data is not provided in the search results. Its properties as a small molecule antagonist suggest it is likely orally bioavailable.
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| Toxicity/Toxicokinetics |
Specific toxicity data for GLPG0974 is not provided in the search results. As a selective FFA2 antagonist, its toxicity profile would be related to its mechanism of action. Standard toxicological studies would be required for clinical development.
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| References | |
| Additional Infomation |
GLPG-0974 is being investigated in the clinical trial NCT01721980 (GLPG0974 multiple escalation dose study in healthy subjects).
GLPG0974 is a potent and selective FFA2/GPR43 antagonist that inhibits neutrophil migration and activation. It has potential for treating inflammatory diseases. It is a research compound and has not been approved for clinical use. |
| Molecular Formula |
C25H25N2O4SCL
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|---|---|
| Molecular Weight |
484.995
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| Exact Mass |
484.122
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| Elemental Analysis |
C, 61.91; H, 5.20; Cl, 7.31; N, 5.78; O, 13.20; S, 6.61
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| CAS # |
1391076-61-1
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| Related CAS # |
(S)-GLPG0974;2326220-69-1
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| PubChem CID |
57520598
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
4.3
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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-RUZDIDTESA-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-/m1/s1
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| Chemical Name |
4-[[(2R)-1-(1-benzothiophene-3-carbonyl)-2-methylazetidine-2-carbonyl]-[(3-chlorophenyl)methyl]amino]butanoic acid
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| Synonyms |
GLPG-0974; GLPG 0974; GLPG0974
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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 : ~200 mg/mL (~412.37 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 5 mg/mL (10.31 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 50.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to 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 mg/mL (10.31 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 50.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 5 mg/mL (10.31 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0619 mL | 10.3093 mL | 20.6186 mL | |
| 5 mM | 0.4124 mL | 2.0619 mL | 4.1237 mL | |
| 10 mM | 0.2062 mL | 1.0309 mL | 2.0619 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
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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