Metribolone (Synonyms: r1881) |
| رقم الكتالوجGC19800 |
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.
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Cas No.: 965-93-5
Sample solution is provided at 25 µL, 10mM.
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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[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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