| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 100mg | |||
| Other Sizes |
| Targets |
GLPG0492 R enantiomer selectively targets the androgen receptor (AR), a nuclear receptor that mediates the biological effects of androgens such as testosterone and dihydrotestosterone. As a selective androgen receptor modulator (SARM), the compound binds to AR with high affinity and tissue selectivity, promoting anabolic activity in muscle and bone while minimizing androgenic side effects in other tissues (e.g., prostate, skin, hair follicles). The R-enantiomer of GLPG0492 represents the specific stereoisomer that may exhibit distinct potency, selectivity, and pharmacokinetic properties compared to the racemic mixture or S-enantiomer. The compound is used to study muscle wasting and sarcopenia.
|
|---|---|
| ln Vitro |
In vitro, GLPG0492 R enantiomer acts as a selective androgen receptor modulator, binding to the androgen receptor and activating AR-mediated gene transcription. The compound promotes the expression of anabolic genes involved in muscle protein synthesis and growth, while showing reduced activity in tissues associated with androgenic side effects. In cellular assays using muscle cells (myotubes), GLPG0492 R enantiomer stimulates myotube hypertrophy and increases protein synthesis. The R-enantiomer may exhibit different potency and selectivity compared to the S-enantiomer or racemic mixture. The compound's in vitro profile supports its use as a research tool for studying SARM pharmacology and muscle biology.
|
| ln Vivo |
In vivo, GLPG0492 R enantiomer is used in research to study muscle wasting, sarcopenia, and cachexia. The compound could be effective in decreasing muscle loss in conditions associated with muscle atrophy. As a selective androgen receptor modulator, GLPG0492 promotes anabolic activity in muscle and bone while minimizing androgenic side effects. The R-enantiomer may exhibit improved pharmacokinetic properties and tissue selectivity compared to other forms. However, specific in vivo efficacy data for the R-enantiomer are limited in publicly available sources. The compound is intended for research use only.
|
| Enzyme Assay |
In vitro receptor binding assays for GLPG0492 R enantiomer are performed using recombinant human androgen receptor (AR) protein or cell lysates expressing AR. Radiolabeled ligands such as [3H]-R1881 (methyltrienolone) are used. The receptor is incubated with varying concentrations of GLPG0492 R enantiomer in assay buffer at 4degC for 2-4 hours. Bound and free radioligands are separated by charcoal-dextran precipitation or hydroxyapatite adsorption. Bound radioactivity is quantified by liquid scintillation counting. Ki values are calculated using the Cheng-Prusoff equation. Selectivity is assessed against other nuclear receptors including estrogen, progesterone, and glucocorticoid receptors.
|
| Cell Assay |
Cellular assays for GLPG0492 R enantiomer are performed using muscle cell lines such as C2C12 myoblasts or L6 myotubes, as well as prostate cancer cell lines expressing AR (e.g., LNCaP). Cells are cultured in appropriate medium and seeded in 6- or 96-well plates. Cells are treated with serial dilutions of GLPG0492 R enantiomer (0.001-10 microM) for 24-72 hours. AR-mediated transcriptional activity is assessed using a luciferase reporter assay with an androgen response element (ARE)-containing promoter. Myotube hypertrophy is assessed by measuring myotube diameter and fusion index. Protein synthesis is measured by [3H]-leucine incorporation. Cell proliferation is assessed by MTT assay. EC₅0 values for AR activation are calculated.
|
| Animal Protocol |
In vivo animal studies for GLPG0492 R enantiomer are conducted in rodent models of muscle wasting and sarcopenia. Male rats or mice are administered GLPG0492 orally at doses of 0.1-10 mg/kg daily for 2-4 weeks. Muscle mass (gastrocnemius, quadriceps, soleus) and muscle strength (grip strength, rotarod) are assessed. Bone mineral density is measured by DXA. Serum testosterone levels and prostate weight are monitored to assess androgenic side effects. Pharmacokinetic parameters (Cmax, Tmax, AUC, t1/2) are determined from plasma samples by LC-MS/MS. Efficacy is compared to vehicle control and standard SARMs.
|
| ADME/Pharmacokinetics |
GLPG0492 R enantiomer (CAS#: 1215085-93-0) has molecular formula C1₉H14F3N3O3 and molecular weight 389.33. The compound is the R-enantiomer of GLPG0492, a novel selective androgen receptor modulator (SARM). It is used as a research compound in studies of muscle wasting, sarcopenia, cachexia, and selective androgen receptor modulation mechanisms. The compound is supplied as a research chemical for laboratory use only. Storage should be at -20degC, protected from light and moisture. The compound is soluble in DMSO.
|
| References |
|
| Additional Infomation |
GLPG0492 R enantiomer (CAS#: 1215085-93-0) is the R-enantiomer of GLPG0492, a novel selective androgen receptor modulator (SARM). SARMs are a class of compounds that selectively target androgen receptors in muscle and bone, promoting anabolic activity (muscle growth, bone density) while minimizing androgenic side effects (prostate stimulation, virilization). GLPG0492 is widely used as a research compound in studies of muscle wasting, sarcopenia, cachexia, and selective androgen receptor modulation mechanisms. As of the current date, GLPG0492 R enantiomer remains a preclinical research compound and is not approved for clinical use.
|
| Molecular Formula |
H3N
|
|---|---|
| Molecular Weight |
17.0305197238922
|
| Exact Mass |
389.099
|
| CAS # |
1215085-93-0
|
| Related CAS # |
GLPG0492;1215085-92-9
|
| PubChem CID |
59317173
|
| Appearance |
White to off-white solid powder
|
| LogP |
2.866
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
7
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
28
|
| Complexity |
683
|
| Defined Atom Stereocenter Count |
1
|
| SMILES |
CN1C(=O)N(C(=O)[C@]1(CO)C2=CC=CC=C2)C3=CC(=C(C=C3)C#N)C(F)(F)F
|
| InChi Key |
VAJGULUVTFDTAS-SFHVURJKSA-N
|
| 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-/m0/s1
|
| Chemical Name |
4-[(4R)-4-(hydroxymethyl)-3-methyl-2,5-dioxo-4-phenylimidazolidin-1-yl]-2-(trifluoromethyl)benzonitrile
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~256.85 mM)
|
|---|---|
| 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 | 58.7199 mL | 293.5995 mL | 587.1991 mL | |
| 5 mM | 11.7440 mL | 58.7199 mL | 117.4398 mL | |
| 10 mM | 5.8720 mL | 29.3600 mL | 58.7199 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
