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R1881

Cat. No. M8128
R1881 Structure
Synonym:

Metribolone

Size Price Availability Quantity
5mg USD 80  USD80 In stock
10mg USD 160  USD160 In stock
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Quality Control & Documentation
Biological Activity

R1881, also known as methyltrienolone, is a synthetic androgen being a 17α-alkylated nandrolone (19-nortestosterone) derivative. R1881 (Metribolone) binds strongly to the androgen receptor and has therefore also been used as an affinity label for this receptor in the prostate and in prostatic tumors. R1881 (Metribolone) is the gold standard AR agonist. Androgen receptors (ARs) are nuclear hormone receptors/transcription factors.

Product Citations
Chemical Information
Molecular Weight 284.39
Formula C19H24O2
CAS Number 965-93-5
Solubility (25°C) DMSO 10 mg/mL
Storage 2-8°C, dry, sealed
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Saeid Nekoonam, et al. Roles of methyltrienolone (R1881) in AKTs and AR expression patterns of cultured granulosa-lutein cells

[2] Samir Koirala, et al. Prolactin/Stat5 and androgen R1881 coactivate carboxypeptidase-D gene in breast cancer cells

[3] Armelle-Natsuo Takeda, et al. The synthetic androgen methyltrienolone (r1881) acts as a potent antagonist of the mineralocorticoid receptor

[4] D J Levinson, et al. Characterization of a [3H]methyltrienolone (R1881) binding protein in rat liver cytosol

[5] L F Fanjul, et al. R1881 regulation of steroidogenesis in cultured testicular cells

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Keywords: R1881, Metribolone supplier, Androgen Receptor, inhibitors, activators


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