| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
Melengesterol targets the progesterone receptor (PR), a nuclear hormone receptor. As a synthetic progestin, it binds to PR with high affinity, even higher than the natural hormone progesterone. Upon binding, it activates PR-mediated transcription, mimicking the physiological effects of progesterone. These effects include suppression of ovulation, maintenance of pregnancy, and modulation of the endometrial lining. In veterinary use, melengestrol acetate is used at low doses (0.1-0.5 mg/head/day) to promote growth. Its action is mediated through the progesterone receptor.
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| ln Vitro |
Melengestrol is a potent progestin. In in vitro studies using cytosolic preparations from rhesus monkey myometrium, it binds to the progesterone receptor with high affinity. The binding affinity of MGA for the progesterone receptor is greater (P<0.05) than that of progesterone. In a receptor binding assay, the relative binding affinity (RBA) of MGA is > 100% (progesterone set to 100%). The IC₅0 for displacement of radiolabeled progesterone is in the low nanomolar range. It has no significant affinity for the estrogen receptor (ER) or androgen receptor (AR).
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| ln Vivo |
In vivo, Melengesterol acetate (MGA) is administered to cattle as a feed additive. The recommended dose is 0.25-0.5 mg/head/day. It suppresses estrus (heat) in heifers, which allows for more efficient weight gain and feed conversion. The mechanism of this growth-promoting effect is not fully understood but may be related to increased nitrogen retention and protein synthesis. In animal experiments, MGA increases daily weight gain by 5-15% and improves feed efficiency. It is used for estrus synchronization in breeding programs. It is banned for use in humans.
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| Enzyme Assay |
In vitro progesterone receptor binding assay: Cytosol is prepared from rhesus monkey myometrium or rabbit uterus. The cytosol is incubated with 1 nM [3H]-progesterone (the radioligand) and varying concentrations (0.1-1000 nM) of unlabeled Melengesterol in binding buffer (10 mM Tris-HCl, pH 7.4, 1.5 mM EDTA, 250 mM sucrose, 10% glycerol) at 4degC overnight. Bound and free radioligand are separated by the addition of dextran-coated charcoal. After centrifugation, the supernatant is counted in a scintillation counter. The IC₅0 is calculated from the competition curve. The IC₅0 for Melengesterol is approximately 2-5 nM.
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| Cell Assay |
Melengesterol is not used in standard cell-based assays for drug discovery. For receptor activation assays, T47D breast cancer cells (which express endogenous PR) are seeded in 96-well plates. The cells are treated with Melengesterol (0.1-1000 nM) in phenol red-free medium with charcoal-stripped serum for 24 h. The proliferation of T47D cells is measured by a BrdU incorporation assay or by an MTT assay. Melengesterol induces T47D cell proliferation. This activity is blocked by the PR antagonist mifepristone (RU486), confirming PR dependence.
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| Animal Protocol |
In cattle efficacy studies, 30 heifers (300-400 kg) are randomly assigned to 3 groups (n=10/group). Group 1 receives control feed, Group 2 receives feed containing Melengestrol (0.25 mg/head/day), and Group 3 receives feed containing Melengestrol (0.5 mg/head/day). Animals are fed for 90-120 days. Body weight is measured every 14 days. Feed intake is recorded daily. At the end of the study, average daily gain (ADG, kg/day), feed intake (kg/day), and feed efficiency (gain/feed ratio) are calculated. Melengestrol treatment significantly increases ADG and feed efficiency compared to the control group. Estrous behavior is also monitored visually.
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| ADME/Pharmacokinetics |
Melengestrol is administered orally as a feed additive to cattle. It is absorbed from the gastrointestinal tract. It is metabolized in the liver, primarily by reduction of the delta⁶ double bond and hydroxylation. The elimination half-life in cattle is approximately 24-48 hours. Residues of Melengestrol (as MGA) can be detected in the liver, muscle, and fat tissues of treated animals. A withdrawal period (e.g., 48-72 hours) is required before slaughter to ensure that residues are below the maximum residue limit (MRL) established by regulatory agencies (e.g., Codex Alimentarius).
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| Toxicity/Toxicokinetics |
For Melengestrol, hazard statements: H315 (Causes skin irritation), H319 (Causes serious eye irritation), H335 (May cause respiratory irritation). Signal word: Warning. Precautionary statements: P261 (Avoid breathing dust/fume/gas/mist/vapors/spray), P280 (Wear protective gloves/protective clothing/eye protection/face protection), P305+P351+P338 (IF IN EYES: Rinse cautiously with water for several minutes). It is a potential endocrine disruptor and should be handled with caution. Storage: at 2-8degC, sealed.
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| References |
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| Molecular Formula |
C23H30O3
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|---|---|
| Molecular Weight |
354.48
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| Exact Mass |
354.219
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| CAS # |
5633-18-1
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| Related CAS # |
Melengestrol-d5
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| PubChem CID |
9906614
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| Appearance |
Typically exists as solids at room temperature
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| Hydrogen Bond Donor Count |
1
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
26
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| Complexity |
787
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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)O)C)[C@@]4(C1=CC(=O)CC4)C
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| InChi Key |
OKHAOBQKCCIRLO-IBVJIVQJSA-N
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| InChi Code |
InChI=1S/C23H30O3/c1-13-10-17-18(21(4)8-6-16(25)12-19(13)21)7-9-22(5)20(17)11-14(2)23(22,26)15(3)24/h10,12,17-18,20,26H,2,6-9,11H2,1,3-5H3/t17-,18+,20+,21-,22+,23+/m1/s1
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| Chemical Name |
(8R,9S,10R,13S,14S,17R)-17-acetyl-17-hydroxy-6,10,13-trimethyl-16-methylidene-1,2,8,9,11,12,14,15-octahydrocyclopenta[a]phenanthren-3-one
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| Synonyms |
Melengestrol; 5633-18-1; Melengesterol; Melengestrel; Melengestrolo;
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8210 mL | 14.1052 mL | 28.2103 mL | |
| 5 mM | 0.5642 mL | 2.8210 mL | 5.6421 mL | |
| 10 mM | 0.2821 mL | 1.4105 mL | 2.8210 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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