2. Vitamin D Related/Nuclear Receptor
  3. Androgen Receptor
  4. GLPG0492

GLPG0492 is an orally active, non-steroidal selective androgen receptor modulator. GLPG0492 exerts functional transactivation by binding to the ligand-binding domain of the receptor, exhibiting preferential partial agonist activity in muscle and bone tissues with low activity in reproductive tissues. GLPG0492 effectively counteracts muscle atrophy-related pathways, significantly enhances muscle strength, maintains motor ability, reduces fibrosis and improves electrophysiological parameters. GLPG0492 prevents immobilization-induced muscle atrophy and regulates muscle mass homeostasis, serving as a valuable tool compound for studies on Duchenne muscular dystrophy, muscle loss and various types of disuse musculoskeletal atrophy.

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GLPG0492

GLPG0492 Chemical Structure

CAS No. : 1215085-92-9

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Based on 7 publication(s) in Google Scholar

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GLPG0492 Related Antibodies

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Description

GLPG0492 is an orally active, non-steroidal selective androgen receptor modulator. GLPG0492 exerts functional transactivation by binding to the ligand-binding domain of the receptor, exhibiting preferential partial agonist activity in muscle and bone tissues with low activity in reproductive tissues. GLPG0492 effectively counteracts muscle atrophy-related pathways, significantly enhances muscle strength, maintains motor ability, reduces fibrosis and improves electrophysiological parameters. GLPG0492 prevents immobilization-induced muscle atrophy and regulates muscle mass homeostasis, serving as a valuable tool compound for studies on Duchenne muscular dystrophy, muscle loss and various types of disuse musculoskeletal atrophy[1][2][3][4].

In Vitro

GLPG0492 (10-12-10-5 M) acts as a weak androgen agonist in yeast androgen screening assays, with an EC50 of 1.30 × 10-6 M[1].
GLPG0492 (10-11-10-5 M; 24 h) acts as an androgen agonist in human PC3 (AR) 2 prostate cancer cells, with an EC50 of 1.24 × 10-8 M, and this agonistic activity is antagonized by the antiandrogen drug bicalutamide (HY-14249)[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

GLPG0492 Related Antibodies
In Vivo

GLPG0492 (30 mg/kg; s.c.; once daily, 6 days per week; for 4 consecutive weeks) significantly improves in vivo forelimb strength and exercise endurance in mdx mice after exercise, enhances diaphragmatic contractile function, reduces diaphragmatic fibrosis, and improves the levels of EDL muscle cell injury markers[2].
GLPG0492 (0.3-30 mg/kg; s.c.; once daily, 6 days per week for 12 weeks) significantly enhances long-term forelimb strength and exercise endurance in mdx mice after exercise, improves the functions of the diaphragm and EDL muscle, reduces the degeneration-regeneration cycle and fibrosis of the diaphragm, and ameliorates cell damage markers in the EDL muscle, with a plateau effect often observed at low doses[2].
GLPG0492 (0.3-30 mg/kg; s.c.; 6 days per week; for 4 to 12 weeks) significantly increases forelimb grip strength, maintains running capacity, improves muscle electrophysiological and histological parameters, and exhibits a dose-dependent therapeutic effect in exercised mdx mice (a model of Duchenne muscular dystrophy)[3].
GLPG0492 (0.3-10 mg/kg; s.c.; once daily for 7 consecutive days) dose-dependently alleviates hindlimb immobilization-induced muscle atrophy in male BALB/cj mice; at doses of 3 and 10 mg/kg/day, it exerts maximal improving effects on muscle mass and myofiber size, without causing damage to reproductive tissues, and regulates key muscle atrophy signaling pathways related to mitochondrial bioenergetics and plasma metabolic markers[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/10ScSn-Dmdmdx/J mice with Duchenne muscular dystrophy (male, 4-5 weeks old, homogeneous for body weight, forelimb force, exercise resistance, Duchenne muscular dystrophy model with treadmill exercise)[2]
Dosage: 0.3 mg/kg; 3 mg/kg; 30 mg/kg
Administration: s.c.; once daily, 6 days/week; 12 weeks
Result: Increased absolute and body weight-normalized forelimb force at T4, T8, and T12 compared to vehicle controls across all doses; 30 mg/kg dose produced the highest absolute forelimb force at T12.\nIncreased treadmill running distance at T4, T8, and T12 compared to vehicle controls across all doses; 3 mg/kg dose maintained maximal activity over 12 weeks, while 0.3 and 3 mg/kg doses were more effective than 30 mg/kg at T4.\nIncreased diaphragm twitch and tetanic tension with 41% and 50% recovery scores relative to wild-type mice at 0.3 mg/kg dose; higher doses showed non-significant upward trends.\nIncreased EDL twitch force at 3 and 30 mg/kg doses; all doses showed non-significant increases in EDL tetanic tension; 3 and 30 mg/kg doses produced wild-type-like EDL resistance to fatigue, while 0.3 and 3 mg/kg doses partially protected against eccentric contraction force drop (non-significant); all doses shifted EDL muscle fibre mechanical threshold voltages to more positive values, reduced rheobase voltage, shortened time constant to reach rheobase, and increased gm compared to vehicle controls.\nReduced diaphragm centrally nucleated fibres from 48 ± 2.4% (vehicle) to 41 ± 1.8% at 0.3 mg/kg dose; all doses reduced total and active TGF-β1 levels in the diaphragm with an inverse dose-dependent relationship (0.3 mg/kg most effective).\nShowed no significant effect on plasma CK or LDH levels at any dose; 3 mg/kg dose resulted in significantly lower body weight gain compared to other groups; no significant effect on trabecular bone structural parameter (BV/TV) observed.
Animal Model: mdx mice with Duchenne Muscular Dystrophy[3]
Dosage: 30 mg/kg (4-week study); 0.3-30 mg/kg (up to 12-week time- and dose-dependent study)
Administration: s.c.; 6 days per week; 4 weeks; s.c.; up to 12 weeks
Result: Increased maximal forelimb grip strength to 0.168 kg.
Preserved running performance over 4 weeks, while comparator- or vehicle-treated animals showed 30-50% increased fatigue.
Induced a modest but statistically significant increase in diaphragm tetanic tension. Decreased non-muscular tissue area in the diaphragm (greater than that seen with nandrolone).
Significantly improved extensor digitorum longus chloride conductance and mechanical threshold.
Confirmed effect on mouse strength and resistance to fatigue in a separate time- and dose-dependent study, and showed significant efficacy of lower doses on in vivo and ex vivo functional parameters.
Animal Model: BALB/cj (male, 10 weeks old, unilateral hindlimb plaster casting for 7 days)[4]
Dosage: 0.3-10 mg/kg/day
Administration: s.c.; daily; 7 days
Result: Reduced immobilization-induced gastrocnemius atrophy dose-dependently, with maximal significant effect at 3 and 10 mg/kg/day.
Caused a statistically significant increase in contralateral (non-immobilized) leg gastrocnemius weight at 3 mg/kg/day compared to intact animals.
Increased mean muscle fiber cross-sectional area (FCSA) in immobilized gastrocnemius muscle dose-dependently, with significant effects at all tested doses relative to vehicle-treated immobilized mice, with effects comparable to testosterone propionate and a trend toward greater activity on slow-twitch fibers.
Significantly inhibited immobilization-induced upregulation of MurF1, FoxO1, Myogenin, and IL1β gene expression in tibialis muscle at 10 mg/kg/day.
Significantly increased PGC-1α gene expression and significantly decreased PGC-1α4 gene expression in tibialis muscle at 10 mg/kg/day relative to vehicle-treated immobilized mice.
Did not cause a significant increase in prostate weight or alter circulating testosterone levels at any tested dose. Significantly increased serum levels of glutamine, pyruvate, citrate, fumarate, 3-hydroxybutyrate, acetate, acetone, mannose, and O-acetylcarnitine at 10 mg/kg/day relative to vehicle-treated immobilized mice.
Clinical Trial
Molecular Weight

389.33

Formula

C19H14F3N3O3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

N#CC1=CC=C(N(C(N(C)[C@]2(CO)C3=CC=CC=C3)=O)C2=O)C=C1C(F)(F)F
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 50 mg/mL (128.43 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (6.42 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (6.42 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.85%

SDS (251 KB)

COA (255 KB) LCMS (94 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.5685 mL 12.8426 mL 25.6852 mL 64.2129 mL
5 mM 0.5137 mL 2.5685 mL 5.1370 mL 12.8426 mL
10 mM 0.2569 mL 1.2843 mL 2.5685 mL 6.4213 mL
15 mM 0.1712 mL 0.8562 mL 1.7123 mL 4.2809 mL
20 mM 0.1284 mL 0.6421 mL 1.2843 mL 3.2106 mL
25 mM 0.1027 mL 0.5137 mL 1.0274 mL 2.5685 mL
30 mM 0.0856 mL 0.4281 mL 0.8562 mL 2.1404 mL
40 mM 0.0642 mL 0.3211 mL 0.6421 mL 1.6053 mL
50 mM 0.0514 mL 0.2569 mL 0.5137 mL 1.2843 mL
60 mM 0.0428 mL 0.2140 mL 0.4281 mL 1.0702 mL
80 mM 0.0321 mL 0.1605 mL 0.3211 mL 0.8027 mL
100 mM 0.0257 mL 0.1284 mL 0.2569 mL 0.6421 mL
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GLPG0492 Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GLPG04921215085-92-9GLPG 0492GLPG-0492Androgen Receptorandrogen receptor ligand binding domainmale BALB/cj micemusculoskeletal atrophydiaphragm fibrosishuman PC3(AR)2 prostate carcinoma cellsmdx miceDuchenne muscular dystrophymuscle atrophy pathwaysandrogen receptor signalingmuscular dystrophyInhibitorinhibitorinhibit

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