| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 100mg | |||
| 250mg | |||
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| Targets |
Glucocorticoid receptor (GR) as an agonist; also inhibits testicular aromatase.
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|---|---|
| ln Vitro |
Paramethasone Acetate is a glucocorticoid receptor agonist with anti-inflammatory and immunosuppressant activity. It directly inhibits testicular aromatase, reducing estradiol synthesis. The compound suppresses basal and midcycle luteinizing hormone surges in female animals and blocks estrogen synthesis. Paramethasone acetate is approximately one-third as potent as dexamethasone and is 2.1 times more potent than prednisone. The compound also affects androstenedione and estradiol in male animals.
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| ln Vivo |
In vivo, Paramethasone Acetate suppresses basal and midcycle luteinizing hormone surges in female animals and blocks estrogen synthesis. It also affects dihydrotestosterone, androstenedione, and estradiol in male animals. As a glucocorticoid, it has broad anti-inflammatory and immunosuppressant effects. The more potent glucocorticoids such as paramethasone and dexamethasone are excreted more slowly in the urine and feces, and are less metabolized. Radioactivities of all labeled synthetic glucocorticoids were recovered more in the liver, kidney, adrenal gland, and lung than in the muscle, subcutaneous tissue, spleen, and brain.
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| Enzyme Assay |
Glucocorticoid receptor binding affinity is assessed using in vitro radioligand binding assays with recombinant GR or GR-containing cell lysates. Agonist activity is evaluated using reporter gene assays in GR-responsive cells (e.g., GR-Luciferase reporter assays). Aromatase inhibition is assessed using in vitro enzyme assays measuring the conversion of androstenedione or testosterone to estradiol using human placental or recombinant aromatase, with product quantification by ELISA or radiometric assays.
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| Cell Assay |
Cellular activity is evaluated in immune cells (e.g., PBMCs, macrophages, T cells) or other glucocorticoid-responsive cells. Cells are treated with Paramethasone Acetate at various concentrations (typically 0.001-100 μM) for appropriate time periods (4-24 hours for cytokine production, 24-72 hours for gene expression). Inflammatory cytokine production (TNFα, IL-1β, IL-6, IL-8) is measured by ELISA or multiplex assays. GR target gene expression (e.g., GILZ, MKP-1, glucocorticoid-induced leucine zipper) is measured by qRT-PCR. Aromatase activity is assessed in relevant cell types (e.g., granulosa cells, placental cells, adipocytes) by measuring estradiol production by ELISA. NF-κB and AP-1 transcriptional activity may be assessed by reporter assays.
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| Animal Protocol |
In vivo efficacy is studied in animal models of inflammation (carrageenan-induced paw edema, croton oil-induced ear edema), autoimmune diseases (EAE, collagen-induced arthritis), and allergic diseases (asthma, atopic dermatitis). Paramethasone Acetate is administered orally, intraperitoneally, or topically at doses determined from pharmacokinetic and tolerability studies. Inflammatory markers (cytokine levels, immune cell infiltration), disease severity scores, and hormone levels (luteinizing hormone, estradiol, testosterone) are assessed. Pharmacodynamic markers include GR target gene expression and NF-κB activity in target tissues. The compound is used clinically as an anti-inflammatory medication.
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| ADME/Pharmacokinetics |
Paramethasone Acetate has a molecular formula of C24H31FO6 and a molecular weight of 434.50 g/mol. CAS Number: 1597-82-6. Purity: typically ≥98% by HPLC. It is a synthetic glucocorticoid. The compound is orally active and long-acting. Solubility: soluble in DMSO and organic solvents; poor water solubility. Storage: store at room temperature or -20°C for long-term stability, protected from light and moisture. Detailed pharmacokinetic parameters are available from clinical pharmacology studies. The more potent glucocorticoids such as paramethasone are excreted more slowly in the urine and feces, and are less metabolized.
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| Toxicity/Toxicokinetics |
Safety data for Paramethasone Acetate are well-established from clinical use. As a glucocorticoid, potential side effects include immunosuppression, metabolic disturbances (hyperglycemia, hyperlipidemia), osteoporosis, adrenal suppression, Cushing's syndrome, hypertension, fluid retention, and endocrine effects. The compound should be handled with appropriate safety precautions as a potent active pharmaceutical ingredient. Use personal protective equipment (gloves, lab coat, safety goggles) and adequate ventilation. Avoid inhalation, ingestion, and skin contact. The compound is for research use and prescription use only. Consult the material safety data sheet (MSDS) for detailed safety information.
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| Additional Infomation |
Acetaminophen acetate is a corticosteroid hormone.
Paramethasone Acetate is an approved glucocorticoid medication used for the treatment of various inflammatory and autoimmune conditions. It is a synthetic, fluorinated corticosteroid. The compound is used to investigate cytokine modulation, inflammatory mediator release, and glucocorticoid receptor signaling pathways in research. Paramethasone acetate is approximately one-third as potent as dexamethasone and is 2.1 times more potent than prednisone. The more potent glucocorticoids such as paramethasone and dexamethasone are excreted more slowly in the urine and feces, and are less metabolized. Radioactivities of labeled synthetic glucocorticoids were recovered more in the liver, kidney, adrenal gland, and lung than in other tissues. |
| Molecular Formula |
C24H31FO6
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|---|---|
| Molecular Weight |
434.5
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| Exact Mass |
434.21
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| Elemental Analysis |
C, 66.34; H, 7.19; F, 4.37; O, 22.09
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| CAS # |
1597-82-6
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| PubChem CID |
443928
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| Appearance |
White to light yellow solid powder
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| Density |
1.29 g/cm1.29 g/cm3
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| Boiling Point |
584.2ºC at 760 mmHg
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| Melting Point |
>148°C (dec.) (lit.)
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| Flash Point |
307.1ºC
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| Vapour Pressure |
4.42E-16mmHg at 25°C
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| Index of Refraction |
1.569
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| LogP |
2.322
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
31
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| Complexity |
895
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| Defined Atom Stereocenter Count |
9
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| SMILES |
CC(OCC([C@]1([C@H](C)C[C@H]2[C@@H]3C[C@H](F)C4=CC(C=C[C@]4(C)C3[C@H](C[C@]12C)O)=O)O)=O)=O
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| InChi Key |
HYRKAAMZBDSJFJ-LFDBJOOHSA-N
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| InChi Code |
InChI=1S/C24H31FO6/c1-12-7-16-15-9-18(25)17-8-14(27)5-6-22(17,3)21(15)19(28)10-23(16,4)24(12,30)20(29)11-31-13(2)26/h5-6,8,12,15-16,18-19,21,28,30H,7,9-11H2,1-4H3/t12-,15+,16+,18+,19+,21-,22+,23+,24+/m1/s1
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| Chemical Name |
[2-[(6S,8S,9S,10R,11S,13S,14S,16R,17R)-6-fluoro-11,17-dihydroxy-10,13,16-trimethyl-3-oxo-7,8,9,11,12,14,15,16-octahydro-6H-cyclopenta[a]phenanthren-17-yl]-2-oxoethyl] acetate
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| Synonyms |
Monocortin; UNII-8X50N88ZDP; PARAMETHASONE ACETATE; 1597-82-6; Monocortin; Haldrone; Paramethasone 21-acetate; Paramethasone Acetate
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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 | 2.3015 mL | 11.5075 mL | 23.0150 mL | |
| 5 mM | 0.4603 mL | 2.3015 mL | 4.6030 mL | |
| 10 mM | 0.2301 mL | 1.1507 mL | 2.3015 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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