| Size | Price | Stock | Qty |
|---|---|---|---|
| 100mg |
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| Other Sizes |
| Targets |
Melengestrol acetate targets the progesterone receptor, functioning as a potent agonist. It binds to progesterone receptors with high affinity relative to progesterone, as demonstrated in rhesus monkey myometrial cytosolic preparations. By activating the progesterone receptor, the compound modulates the transcription of progesterone-responsive genes involved in reproductive function, including estrus suppression. In veterinary medicine, it is used as a growth promotant and for estrus synchronization in livestock.
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| ln Vitro |
In vitro, melengestrol acetate demonstrates potent progesterone receptor agonist activity. It binds to progesterone receptors with high affinity relative to progesterone in rhesus monkey myometrial cytosolic preparations. The compound's activity is assessed in cell-based reporter assays using progesterone response element (PRE)-luciferase constructs and in binding assays using progesterone receptor preparations. It has been used in the treatment of various conditions, though primarily in veterinary applications. Its progestational activity is well characterized.
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| ln Vivo |
AT3 tumor growth is inhibited by megenestrol acetate (sc; 10 mg/kg; 9 days) by about 53%. Additionally, it results in a decrease of the seminal vesicles and a 54% weight loss of the ventral prostate in adult male CCFl rats[1]. In rats, oral treatment of meleengestrol acetate (10 mg/kg) results in a 58.8% growth inhibition of Dunning R3327-AT3 tumors and a 51.6% reduction in adrenal weight[1].
In vivo, melengestrol acetate suppresses estrus in rats at a dose of 0.1 mg/animal per day. It reduces tumor growth in androgen-dependent models. In veterinary medicine, it is used as a growth promotant and for estrus suppression in livestock. The compound is orally active, supporting convenient administration in animal husbandry. Its effects on reproductive function and growth promotion are well documented. Further studies may explore additional applications. |
| Enzyme Assay |
In vitro enzyme/receptor binding assays for melengestrol acetate typically involve competitive binding experiments using progesterone receptor and radiolabeled or fluorescently labeled progesterone as tracer. The compound's binding affinity to the progesterone receptor is assessed, with IC₅₀ or Kd values determined. Assays are conducted in buffered solutions at physiological pH with appropriate receptor preparations. The compound's agonist activity is confirmed through functional assays measuring PRE-mediated transcriptional activation. Binding affinity is expressed relative to progesterone.
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| Cell Assay |
In vitro cell-based assays for melengestrol acetate utilize cell lines expressing progesterone receptor to assess its agonist activity. Cells are treated with varying concentrations of the compound for 24-48 hours. Progesterone receptor-mediated transcriptional activity is evaluated using reporter gene assays with PRE-luciferase constructs. Progestational activity can also be assessed by measuring the expression of progesterone-responsive genes. Standard cell culture conditions (37°C, 5% CO₂) with appropriate media are employed. Dose-response curves are generated to determine EC₅₀ values.
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| Animal Protocol |
In vivo animal studies with melengestrol acetate typically involve administration to rodent models or livestock to evaluate its progestational and growth-promoting effects. In rats, the compound suppresses estrus at 0.1 mg/animal per day. It reduces tumor growth in androgen-dependent models. In veterinary applications, the compound is used for estrus synchronization and growth promotion in cattle and other livestock. Endpoints include assessment of reproductive function, growth rate, and tumor growth. All procedures must comply with institutional animal care and use guidelines.
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| ADME/Pharmacokinetics |
Melengestrol acetate has a molecular weight of 396.23 g/mol and a molecular formula of C₂₅H₃₂O₄. Its CAS name is 17-(Acetyloxy)-6-methyl-16-methylenepregna-4,6-diene-3,20-dione. It is orally active, supporting convenient administration. The compound is typically stored at -10°C. Its pharmacokinetic properties in veterinary species have been characterized for its approved indications. The compound is used as an analytical standard in environmental chemistry.
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| Toxicity/Toxicokinetics |
Melengestrol acetate is approved for veterinary use as a growth promotant and for estrus suppression. As a veterinary pharmaceutical, it has undergone toxicological evaluation for its approved indications. Common adverse effects in animals may include reproductive effects and other hormonal effects. The compound should be used according to approved veterinary guidelines. Residue monitoring is required in food-producing animals to ensure food safety. The compound is not approved for human use.
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| References | |
| Additional Infomation |
Melengestrol acetate is a corticosteroid hormone. It is a 6-methylprogesterone acetate ester, reported to have glucocorticoid activity and influence estrus. Melengestrol acetate is a progestin-like compound used as a cattle feed additive due to its growth-promoting and estrus-inhibiting effects on heifers. Critics claim that hormones used as growth promoters in cattle may cause mammary cancer. (NCI) It is a 6-methylprogesterone acetate ester, reported to have glucocorticoid activity and influence estrus. See also: Melengestrol (with active moiety); Melengestrol acetate; Tylosin (ingredient); Melengestrol acetate; Monensin (ingredient)... See more...
Melengestrol acetate (CAS#: 2919-66-6) has a molecular formula of C₂₅H₃₂O₄ and a molecular weight of 396.23 g/mol. Its CAS name is 17-(Acetyloxy)-6-methyl-16-methylenepregna-4,6-diene-3,20-dione. It is a highly potent, orally active synthetic steroidal progestin. It binds to progesterone receptors with high affinity relative to progesterone. It is used in veterinary medicine as a growth promotant and for estrus suppression. It suppresses estrus in rats at 0.1 mg/animal per day and reduces tumor growth in androgen-dependent models. This compound is a veterinary pharmaceutical. |
| Molecular Formula |
C25H32O4
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|---|---|
| Molecular Weight |
396.52
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| Exact Mass |
396.23
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| CAS # |
2919-66-6
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| Related CAS # |
Melengestrol acetate-d3;Melengestrol acetate-d6;Melengestrol acetate-d2
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| PubChem CID |
250948
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| Appearance |
White to yellow solid powder
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| Density |
1.1±0.1 g/cm3
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| Boiling Point |
516.1±50.0 °C at 760 mmHg
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| Melting Point |
202-204ºC
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| Flash Point |
221.7±30.2 °C
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| Vapour Pressure |
0.0±1.3 mmHg at 25°C
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| Index of Refraction |
1.555
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| LogP |
4.21
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
29
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| Complexity |
893
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| Defined Atom Stereocenter Count |
6
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| SMILES |
CC1=C[C@@H]2[C@H](CC[C@]3([C@H]2CC(=C)[C@@]3(C(=O)C)OC(=O)C)C)[C@@]4(C1=CC(=O)CC4)C
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| InChi Key |
UDKABVSQKJNZBH-DWNQPYOZSA-N
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| InChi Code |
InChI=1S/C25H32O4/c1-14-11-19-20(23(5)9-7-18(28)13-21(14)23)8-10-24(6)22(19)12-15(2)25(24,16(3)26)29-17(4)27/h11,13,19-20,22H,2,7-10,12H2,1,3-6H3/t19-,20+,22+,23-,24+,25+/m1/s1
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| Chemical Name |
[(8R,9S,10R,13S,14S,17R)-17-acetyl-6,10,13-trimethyl-16-methylidene-3-oxo-1,2,8,9,11,12,14,15-octahydrocyclopenta[a]phenanthren-17-yl] acetate
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| Synonyms |
MELENGESTROL ACETATE; BDH-1921; NSC-70968; BDH1921; NSC70968; 2919-66-6; DTXSID5048184;
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 25 mg/mL (63.05 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (6.30 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.30 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5219 mL | 12.6097 mL | 25.2194 mL | |
| 5 mM | 0.5044 mL | 2.5219 mL | 5.0439 mL | |
| 10 mM | 0.2522 mL | 1.2610 mL | 2.5219 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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