Metribolone (Synonyms: r1881) |
Catalog No.GC19800
One-Click Copy Product Info
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Metribolone (R1881), also known as methyltrienolone, is a synthetic androgen ligand that binds strongly to the androgen receptor (AR) with a Ki value of 0.09nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 965-93-5
Sample solution is provided at 25 µL, 10mM.
Metribolone (R1881), also known as methyltrienolone, is a synthetic androgen ligand that binds strongly to the androgen receptor (AR) with a Ki value of 0.09nM[1]. Metrebolone is an agonist of AR and acts as an antagonist of the mineralocorticoid receptor (MR) in aldosterone target cells[2]. Radiolabeled metrebolone can be used as a tracer for AR [3].
In vitro, metrebolone (0.05-5nM) treated vascular endothelial cells and up-regulated the expression of p53, p21 and p27 proteins by activating the AR/cSrc/AKT/p38/ERK/NFκB signaling pathway, thereby inhibiting the expression of vascular endothelial cells. proliferation[4]. Metrebolone (100nM) treated Calu-3 cells for 30 hours, which promoted the activation of TMPRSS2 without affecting the total expression of TMPRSS2 and significantly increased the expression level of spike protein [5].
In vivo, when metrebolone (1200 µg/day; s.c) treated EDS/GnRHa/rec-hFSH rats, the relative weight of the prostate and seminal vesicles increased well above 100%, while the relative weight of the testes was maintained at 93% [6]. Metrebolone administered 0.5 or 2.5 mg/kg mixed into feed will increase the body weight of male piglets, but not female piglets [7].
References:
[1] Murthy L R, Chang C H, Rowley D R, et al. Physicochemical characterization of the androgen receptor from hyperplastic human prostate[J]. The Prostate, 1984, 5(6): 567-579.
[2] Takeda A N, Pinon G M, Bens M, et al. The synthetic androgen methyltrienolone (r1881) acts as a potent antagonist of the mineralocorticoid receptor[J]. Molecular pharmacology, 2007, 71(2): 473-482.
[3] Raynaud J P, Ojasoo T, Vaché V. Stable and specific tracers[M]//Reproductive Processes and Contraception. Boston, MA: Springer US, 1981: 163-179.
[4] Huo Y N, Yeh S D, Chou C M, et al. Androgen receptor activation inhibits endothelial cell proliferation through an extra-nuclear signaling pathway[C]//Endocrine Abstracts. Bioscientifica, 2017, 49.
[5] Treppiedi D, Marra G, Di Muro G, et al. TMPRSS2 Expression and Activity Modulation by Sex-Related Hormones in Lung Calu-3 Cells: Impact on Gender-Specific SARS-CoV-2 Infection[J]. Frontiers in Endocrinology, 2022, 13: 862789.
[6]Van ROIJEN J H, OOMS M P, WEBER R F A, et al. Comparison of the response of rat testis and accessory sex organs to treatment with testosterone and the synthetic androgen methyltrienolone (R1881)[J]. Journal of andrology, 1997, 18(1): 51-61.
[7]Szumowski P, Vaissaire J P, Theret M. Effect of the anabolic steroid R. 1881 on growth and fattening of young pigs[J]. Recueil de Medecine Veterinaire, 1967, 143: 343-355.
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Cell experiment [1]: |
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Cell lines |
Calu-3 cells |
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Preparation method |
Cells were maintained in this lipophilic hormones-free medium for 7 days, with two medium changes at day 4 and at day 7, before the start of metribolone treatments. For the experiments, cells were treated at day 7 with estradiol (10nM) or Metribolone (100nM) for 30 h in CSS medium. |
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Reaction Conditions |
100nM; 30h |
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Applications |
Metribolone and estradiol promote TMPRSS2 serine protease activation without affecting total TMPRSS2 expression. The expression level of spike protein increased significantly after 100nM Metribolone treatment. |
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Animal experiment [2]: |
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Animal models |
Wistar rats |
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Preparation method |
were substituted daily with varying amounts of TP (50, 100, 200, and 400µg/day) or Metribolone (150, 300, 600, and 1200µg/day). The androgens were injected s.c. in 0.1ml of corn oil. |
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Dosage form |
150, 300, 600, and 1200µg/day; s.c. |
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Applications |
EDS/GnRHa/rec-hFSH animals treated with Metribolone, no difference in relative testis weight . At a dose of 1200µg Metribolone per day, however, the relative prostate and seminal vesicles weights increased well above 100%, whereas relative testis weight was maintained at 93%. |
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References: [1] Treppiedi D, Marra G, Di Muro G, et al. TMPRSS2 Expression and Activity Modulation by Sex-Related Hormones in Lung Calu-3 Cells: Impact on Gender-Specific SARS-CoV-2 Infection[J]. Frontiers in Endocrinology, 2022, 13: 862789. [2] Van ROIJEN J H, OOMS M P, WEBER R F A, et al. Comparison of the response of rat testis and accessory sex organs to treatment with testosterone and the synthetic androgen methyltrienolone (R1881)[J]. Journal of andrology, 1997, 18(1): 51-61. |
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| Cas No. | 965-93-5 | SDF | |
| Synonyms | r1881 | ||
| Formula | C19H24O2 | M.Wt | 284.39 |
| Solubility | ≥50mg/ml in DMSO | Storage | Store at 2-8°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.5163 mL | 17.5815 mL | 35.163 mL |
| 5 mM | 703.3 μL | 3.5163 mL | 7.0326 mL |
| 10 mM | 351.6 μL | 1.7581 mL | 3.5163 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 11 reference(s) in Google Scholar.)