| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 100mg | |||
| Other Sizes |
| Targets |
The primary target of Amebucort is the glucocorticoid receptor (GR). As a synthetic glucocorticoid, it binds to the glucocorticoid receptor, modulating gene expression and leading to anti-inflammatory and immunosuppressive effects. By activating the GR, it can suppress the production of pro-inflammatory cytokines and mediators, reduce immune cell activation, and promote the resolution of inflammation. Its mechanism is similar to other corticosteroids.
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| ln Vitro |
In vitro, Amebucort exhibits anti-inflammatory properties. As a glucocorticoid, its activity would be assessed by its ability to modulate the expression of inflammatory genes in cell-based reporter assays or by measuring its effect on cytokine production in activated immune cells. Its potency and efficacy would be compared to other corticosteroids. These in vitro studies help characterize its mechanism of action and potency.
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| ln Vivo |
In vivo, Amebucort has been studied for its anti-inflammatory activity. It is a synthetic corticosteroid with potential use in the research of inflammatory diseases. Its development for topical anti-inflammatory application suggests it was intended for local administration to treat skin inflammation. Its in vivo efficacy and safety profile would have been evaluated in preclinical and clinical studies. The compound is a discontinued research-phase drug.
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| Enzyme Assay |
In vitro enzyme/receptor binding studies for Amebucort would involve assessing its affinity for the glucocorticoid receptor (GR). This can be done using radioligand binding assays where the compound competes with a labeled glucocorticoid for binding to the GR. The IC₅₀ or Ki value is determined from the competition curve. Its selectivity for the GR over other steroid receptors (e.g., mineralocorticoid, androgen, progesterone) can also be assessed. These protocols are for research purposes only.
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| Cell Assay |
In vitro cell-based assays for Amebucort evaluate its glucocorticoid activity. A common assay uses a reporter cell line transfected with a glucocorticoid response element (GRE)-driven luciferase construct. Cells are treated with the compound, and luciferase activity is measured. Alternatively, its anti-inflammatory activity can be assessed in immune cells (e.g., macrophages or lymphocytes) stimulated with LPS or other activators, and the production of cytokines like TNF-α, IL-6, and IL-1β is measured by ELISA. Cytotoxicity is assessed using standard assays.
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| Animal Protocol |
In vivo animal studies for Amebucort would have used standard models of inflammation. For topical application, models of contact dermatitis or skin inflammation would be appropriate. The compound would be applied topically, and the reduction in ear swelling or skin inflammation would be measured. For systemic inflammation, models like carrageenan-induced paw edema or adjuvant-induced arthritis could be used. The compound would be administered systemically, and the reduction in edema or joint inflammation would be assessed. All procedures must comply with institutional animal care guidelines.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of Amebucort are not detailed in the provided literature. As a topical glucocorticoid, its absorption through the skin would be an important parameter. Its metabolism and systemic bioavailability would also be characterized. The compound has a molecular weight of 488.6 g/mol. Further details on its PK profile would be available from the original research.
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| Toxicity/Toxicokinetics |
The toxicity profile of Amebucort would be typical of glucocorticoids. Chronic use can lead to side effects such as skin atrophy (with topical use), adrenal suppression, hyperglycemia, and immunosuppression. It is classified for research use only and not for human consumption. The compound is discontinued, and its safety profile would have been evaluated in preclinical studies.
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| References | |
| Additional Infomation |
Additional information: Amebucort has the CAS number 83625-35-8. Its molecular formula is C₂₈H₄₀O₇. It is a halogen-free glucocorticoid diester. It was developed for topical anti-inflammatory application but is now a discontinued research-phase compound. Amebucort is a research tool for studying glucocorticoid biology and inflammation. This product is for research use only and is not approved for clinical or therapeutic applications.
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| Molecular Formula |
C28H40O7
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|---|---|
| Molecular Weight |
488.613
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| Exact Mass |
488.277
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| CAS # |
83625-35-8
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| PubChem CID |
3086167
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| Appearance |
White to off-white solid powder
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| Density |
1.2g/cm3
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| Boiling Point |
603.7ºC at 760 mmHg
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| Flash Point |
192.7ºC
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| Index of Refraction |
1.546
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| LogP |
3.949
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
35
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| Complexity |
953
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| Defined Atom Stereocenter Count |
8
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| SMILES |
CCCC(=O)O[C@@]1(CC[C@@H]2[C@@]1(C[C@@H]([C@H]3[C@H]2C[C@@H](C4=CC(=O)CC[C@]34C)C)O)C)C(=O)COC(=O)C
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| InChi Key |
QRRVOCXLQYLNEC-PPJDWOAVSA-N
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| InChi Code |
InChI=1S/C28H40O7/c1-6-7-24(33)35-28(23(32)15-34-17(3)29)11-9-20-19-12-16(2)21-13-18(30)8-10-26(21,4)25(19)22(31)14-27(20,28)5/h13,16,19-20,22,25,31H,6-12,14-15H2,1-5H3/t16-,19-,20-,22-,25+,26-,27-,28-/m0/s1
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| Chemical Name |
[(6S,8S,9S,10R,11S,13S,14S,17R)-17-(2-acetyloxyacetyl)-11-hydroxy-6,10,13-trimethyl-3-oxo-2,6,7,8,9,11,12,14,15,16-decahydro-1H-cyclopenta[a]phenanthren-17-yl] butanoate
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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 : ~100 mg/mL (~204.66 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.26 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 20.8 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 | 2.0466 mL | 10.2331 mL | 20.4662 mL | |
| 5 mM | 0.4093 mL | 2.0466 mL | 4.0932 mL | |
| 10 mM | 0.2047 mL | 1.0233 mL | 2.0466 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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