Dimethandrolone undecanoate
Dimethandrolone undecanoate (7α,11β-Dimethyl-17β-hydroxyestr-4-en-3-one 17-undecanoate) is an orally active androgen. Dimethandrolone undecanoate is cleaved to the active Dimethandrolone, which then mediates androgenic and progestational effects, stimulating ventral prostate and levator ani muscle weight. Dimethandrolone undecanoate suppresses serum LH. Dimethandrolone undecanoate can be used in research on hypogonadism.
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- CAS. Nr.: 366472-45-9
- Formel: C31H50O3
- Molecular Weight:470.73
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
Beschreibung
In Vitro
Dimethandrolone undecanoate (>500 nM for rhPR-A/B; 309 nM for rabbit uterine PR; >1000 nM for ARLBD) has very low binding affinity for rhPR-A, rhPR-B, and ARLBD but binds rabbit uterine PR with an EC50 of 309 nM, indicating no substantial cleavage to DMA in these cytosolic assays[1].
Dimethandrolone undecanoate (10 nM; 20 h) stimulates PR-mediated PRE2-tk-LUC transcription in T47DCO human breast cancer cells, and this response is completely blocked by antiprogestins but only partially by the antiandrogen OH flutamide[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Dimethandrolone undecanoate (0.6-1.2 mg/rat; s.c.; single) produces prolonged androgenic activity with sustained circulating DMA levels in castrate immature male rats[1].
Dimethandrolone undecanoate (12 mg/kg/d; oral; daily; for 14 days) suppresses LH during dosing but not after dosing ended in castrate adult male rats[1].
Dimethandrolone undecanoate (0.4-3.2 mg/d; oral; daily; for 5 days) has dose-dependent progestational activity in estrogen-primed immature female rabbits but does not reach the maximal McPhail response[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague Dawley CD [Crl:CD(SD)] (immature male, 22 days of age, castrated)[1]
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Dosage:0.6 or 1.2 mg/rat
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Administration:s.c.; single injection
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Result:Increases in VP and SV weights occurred during the first 6 weeks of the study and were greater at the 1.2-mg dose; thereafter VP and SV weights declined slowly over 21 weeks but did not involute to the degree seen in vehicle-treated immature castrate male rats.
In rats treated with 1.2 mg DMAU, serum DMA levels were maximal at week 3 and declined gradually to undetectable levels by about week 18.
In rats treated with 0.6 mg DMAU, serum DMA levels were barely detectable over the 21-week period.
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Animal Model:Sprague Dawley CD [Crl:CD(SD)] (adult male, ~300 g, castrated)[1]
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Dosage:12 mg/kg
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Administration:s.c.; single dose
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Result:Serum LH decreased to levels at or close to undetectable by week 1, remained at this level for up to 18 weeks, and increased gradually over the next 12 weeks.
Serum DMA levels peaked at week 1 at about 1000 pg/mL after a single s.c. injection of DMAU and declined very gradually to the limit of detection (112 pg/mL) at 30 weeks.
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Animal Model:Sprague Dawley CD [Crl:CD(SD)] (adult male, ~300 g, castrated)[1]
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Dosage:12 mg/kg/d
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Administration:oral; daily; for 14 days
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Result:Serum LH levels were suppressed to close to undetectable during the dosing interval, but rose to baseline levels by week 3.
Serum DMA levels were 300-400 pg/mL at weeks 1 and 2, but fell precipitously to the limit of detection when dosing ended.
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Animal Model:New Zealand White (HsdOkd:NZW; immature female)[1]
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Dosage:0.4, 0.8, 1.6, or 3.2 mg/d
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Administration:oral; daily; for 5 days
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Result:Produced dose-dependent stimulation of endometrial gland arborization and uterine wet weight.
Uterine weights: 0.4 mg/d, 1.15 g; 0.8 mg/d, 1.31 g; 1.6 mg/d, 1.98 g; 3.2 mg/d, 1.71 g.
Endometrial widths: 0.4 mg/d, 1392 µm; 0.8 mg/d, 1575 µm; 1.6 mg/d, 1768 µm; 3.2 mg/d, 1738 µm.
Myometrial widths: 0.4 mg/d, 142.3 µm; 0.8 mg/d, 168.1 µm; 1.6 mg/d, 217.0 µm; 3.2 mg/d, 196.8 µm.
McPhail index scores: 0.4 mg/d, 0.1; 0.8 mg/d, 1.0; 1.6 mg/d, 2.4; 3.2 mg/d, 2.6.
The response reached a plateau at 1.6 mg/d for DMAU, and a maximal McPhail index score of 4.0 was not achieved even at the highest dose level.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 366472-45-9
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Molecular Weight 470.73
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Formel C31H50O3
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SMILES
C[C@@]12[C@](CC[C@@H]2OC(CCCCCCCCCC)=O)([H])[C@@]3([H])[C@@]([C@H](C1)C)([H])[C@]4([H])C(C[C@H]3C)=CC(CC4)=O
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Synonyms
7α,11β-Dimethyl-17β-hydroxyestr-4-en-3-one 17-undecanoate
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
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Data Sheet (282 KB)
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SDS (252 KB)
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Handling Instructions (2659 KB)
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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