| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg | |||
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| Targets |
Androgen receptor (AR).
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| ln Vitro |
GLPG-0492 is a novel and potent androgen receptor modulator with anabolic activity on muscle. It is a non-steroidal selective androgen receptor modulator (SARM) that can reduce muscle loss while sparing reproductive tissues. GLPG-0492 treatment partially prevents immobilization-induced muscle atrophy and has a tendency to promote muscle fiber hypertrophy in a dose-dependent manner. Specific EC50 values for androgen receptor activation and selectivity data are available from preclinical studies. The compound has the potential to be used for muscle atrophy and possibly for Duchenne muscular dystrophy.
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| ln Vivo |
In vivo, GLPG-0492 has been shown to partially prevent immobilization-induced muscle atrophy and to promote muscle fiber hypertrophy in a dose-dependent manner. The compound has anabolic activity on muscle and can reduce muscle loss while sparing reproductive tissues. Specific dosing regimens and detailed efficacy data are available from preclinical studies. GLPG-0492 has been investigated for the treatment of muscle wasting disorders, including Duchenne muscular dystrophy.
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| Enzyme Assay |
Androgen receptor binding affinity is assessed using in vitro radioligand binding assays with recombinant androgen receptor. Competitive binding with [3H]testosterone or other selective ligands is measured. Androgen receptor activity is assessed using reporter gene assays in cells transfected with androgen receptor and a luciferase reporter. EC50 values are calculated from dose-response curves. Selectivity is evaluated by testing against other nuclear receptors.
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| Cell Assay |
Cellular activity is evaluated in muscle cells (e.g., C2C12 myotubes). Cells are treated with GLPG-0492 at various concentrations (typically 0.001-100 µM) for appropriate time periods. Androgen receptor target gene expression (e.g., myostatin, IGF-1) is measured by qRT-PCR. Protein synthesis is measured by assessing the incorporation of radiolabeled amino acids. Myotube diameter is measured to assess hypertrophy. Selectivity for muscle over reproductive tissues is assessed in relevant cell models.
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| Animal Protocol |
In vivo efficacy is studied in animal models of muscle atrophy, such as immobilization-induced atrophy, denervation-induced atrophy, or cachexia models. GLPG-0492 is administered orally at various doses. Muscle mass (e.g., gastrocnemius, tibialis anterior) is measured. Muscle fiber cross-sectional area is measured histologically. Muscle strength is assessed by grip strength or other functional tests. Reproductive tissue weight (e.g., prostate, seminal vesicles) is measured to assess selectivity.
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| ADME/Pharmacokinetics |
GLPG-0492 has a molecular formula of C19H14F3N3O3 and a molecular weight of 389.33 g/mol. CAS Number: 1215085-92-9. Appearance: White to off-white solid powder. LogP: 2.07. Purity is typically ≥98% by HPLC. The compound is soluble in DMSO (~50 mg/mL). Storage: Powder at -20°C for 3 years or at 4°C for 2 years; in solvent at -80°C for 6 months or at -20°C for 1 month.
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| Toxicity/Toxicokinetics |
Safety data for GLPG-0492 are available from preclinical and clinical studies. As a selective androgen receptor modulator, it may have effects on hormone-dependent tissues. Common adverse events associated with SARMs may include changes in lipid profile, liver enzyme elevations, and suppression of endogenous testosterone production. Specific toxicological profiles are available from preclinical and clinical study reports. The compound is for research use only and not for human therapeutic applications without appropriate regulatory approval.
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| References |
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| Additional Infomation |
Glpg0492 is being studied in the clinical trial NCT01130818 (first-in-human single-increment dose of GLPG0492).
GLPG-0492 is a research tool compound and clinical candidate for studying androgen receptor biology and muscle wasting disorders. It is not approved for clinical use. The compound is a non-steroidal selective androgen receptor modulator (SARM) with anabolic activity on muscle. GLPG-0492 has been investigated for the treatment of muscle atrophy, Duchenne muscular dystrophy, and other conditions involving muscle wasting. Its tissue selectivity for muscle over reproductive tissues makes it a valuable tool for understanding the molecular basis of androgen receptor signaling and for developing therapies that promote muscle growth without undesirable androgenic side effects. |
| Molecular Formula |
C19H14F3N3O3
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|---|---|
| Molecular Weight |
389.3342
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| Exact Mass |
389.098
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| CAS # |
1215085-92-9
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| Related CAS # |
GLPG0492 (R enantiomer);1215085-93-0
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| PubChem CID |
59317190
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| Appearance |
White to off-white solid powder
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| Density |
1.5±0.1 g/cm3
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| Boiling Point |
544.0±60.0 °C at 760 mmHg
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| Flash Point |
282.8±32.9 °C
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| Vapour Pressure |
0.0±1.5 mmHg at 25°C
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| Index of Refraction |
1.627
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| LogP |
2.07
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
28
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| Complexity |
683
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| Defined Atom Stereocenter Count |
1
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| SMILES |
CN1C(=O)N(C(=O)[C@@]1(CO)C2=CC=CC=C2)C3=CC(=C(C=C3)C#N)C(F)(F)F
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| InChi Key |
VAJGULUVTFDTAS-GOSISDBHSA-N
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| InChi Code |
InChI=1S/C19H14F3N3O3/c1-24-17(28)25(14-8-7-12(10-23)15(9-14)19(20,21)22)16(27)18(24,11-26)13-5-3-2-4-6-13/h2-9,26H,11H2,1H3/t18-/m1/s1
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| Chemical Name |
4-[(4S)-4-(hydroxymethyl)-3-methyl-2,5-dioxo-4-phenylimidazolidin-1-yl]-2-(trifluoromethyl)benzonitrile
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| Synonyms |
GLPG0492 GLPG 0492 GLPG-0492
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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 : ≥ 50 mg/mL (~128.43 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.42 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (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 25.0 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: ≥ 2.5 mg/mL (6.42 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (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 25.0 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: ≥ 2.5 mg/mL (6.42 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 | 2.5685 mL | 12.8426 mL | 25.6852 mL | |
| 5 mM | 0.5137 mL | 2.5685 mL | 5.1370 mL | |
| 10 mM | 0.2569 mL | 1.2843 mL | 2.5685 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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