| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 100mg | |||
| Other Sizes |
| Targets |
Glucocorticoid receptor (GR, NR3C1).
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|---|---|
| ln Vitro |
In vitro, prednisolone tebutate binds to the glucocorticoid receptor and modulates gene transcription through both transactivation and transrepression mechanisms. It dampens the inflammatory cytokine cascade, inhibits T cell activation, and suppresses the production of pro-inflammatory mediators such as prostaglandins, leukotrienes, and cytokines. The compound modulates immune responses and inhibits inflammatory mediators through glucocorticoid response element (GRE)-mediated pathways. It is a potent anti-inflammatory agent with efficacy in various in vitro models of inflammation.
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| ln Vivo |
In vivo, prednisolone tebutate has been shown to significantly inhibit inflammatory responses in models such as monosodium urate (MSU) crystal-induced inflammation. Its depot formulation allows for sustained anti-inflammatory activity following injection. The compound is effective in managing various inflammatory and autoimmune conditions in preclinical models. It influences metabolic processes including glucose homeostasis and cholesterol transport.
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| Enzyme Assay |
Receptor binding assays are performed using cytosolic or nuclear extracts from cells expressing glucocorticoid receptors. The assay mixture contains [3H]-dexamethasone or [3H]-prednisolone as the radioligand and varying concentrations of unlabeled prednisolone tebutate (1 nM-100 microM) in binding buffer (10 mM Tris-HCl, pH 7.4, containing 10% glycerol, 1 mM DTT, and 25 mM NaCl). Incubation is carried out at 4degC for 2-4 hours. Bound and free ligand are separated by charcoal adsorption or filtration through DEAE filters. Specific binding is calculated by subtracting non-specific binding (determined in presence of 1000-fold excess unlabeled dexamethasone). Competitive binding curves are analyzed to determine IC₅0 and Ki values.
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| Cell Assay |
Cells (e.g., primary lymphocytes, macrophages, or cell lines such as A549 or U937) are cultured in appropriate medium and treated with prednisolone tebutate at concentrations ranging from 0.1 nM to 100 microM for various time points (1-24 hours). Anti-inflammatory activity is assessed by measuring the inhibition of LPS-stimulated cytokine production (TNF-alpha, IL-6, IL-1beta) using ELISA or multiplex bead-based assays. Glucocorticoid receptor transactivation is evaluated using reporter gene assays (e.g., GRE-luciferase). Cell viability and cytotoxicity are assessed using MTT or LDH assays. EC₅0 values for cytokine inhibition are calculated from dose-response curves.
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| Animal Protocol |
In vivo efficacy is evaluated in animal models of inflammation. For MSU crystal-induced inflammation models, rodents are injected with MSU crystals in the hind paw, and prednisolone tebutate is administered via intramuscular or subcutaneous injection. Paw edema is measured using plethysmometry at multiple time points (e.g., 1, 2, 4, 6, 24 hours post-injection). Inflammatory cell infiltration is assessed by histological analysis of tissue sections. Alternatively, carrageenan-induced paw edema models or adjuvant-induced arthritis models are used to evaluate anti-inflammatory efficacy. Immunosuppressive activity is assessed in models of delayed-type hypersensitivity or experimental autoimmune encephalomyelitis (EAE).
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| ADME/Pharmacokinetics |
Doses typically range from 0.1-10 mg/kg depending on the model and route of administration. The tebutate ester formulation provides a depot effect with prolonged release. Following administration, the compound is hydrolyzed to active prednisolone. Bioavailability is high via parenteral routes. Plasma protein binding exceeds 90% (primarily to corticosteroid-binding globulin and albumin). The half-life is prolonged by the depot formulation. Metabolism occurs primarily in the liver via CYP3A4-mediated oxidation, followed by conjugation and renal excretion.
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| Toxicity/Toxicokinetics |
As a glucocorticoid, prednisolone tebutate is associated with the typical adverse effects of corticosteroid therapy. These may include immunosuppression, increased susceptibility to infections, glucose intolerance, osteoporosis, fluid retention, hypertension, and adrenal suppression with prolonged use. The tebutate ester formulation may reduce the frequency of administration but does not alter the side-effect profile. Long-term use requires monitoring of blood glucose, bone density, and adrenal function. The compound is for research use only and not for human therapeutic use.
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| Additional Infomation |
Prednisolone is a corticosteroid hormone.
See also: Prednisolone (with active ingredient). Prednisolone Tebutate is a corticosteroid ester primarily used in research settings to study glucocorticoid pharmacology and inflammatory pathways. It is not a first-line clinical formulation but serves as a research tool for investigating depot corticosteroid delivery and anti-inflammatory mechanisms. The compound is a derivative of prednisolone, which is widely used clinically for its immunosuppressive and anti-inflammatory effects. Prednisolone and its derivatives are critical in the management of various inflammatory and autoimmune conditions including multiple sclerosis, respiratory distress, and liver diseases. Prednisolone Tebutate is available as a research-grade compound with molecular formula C2₇H3₈O₆ and MW 458.6. |
| Molecular Formula |
C27H38O6
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|---|---|
| Molecular Weight |
458.58702
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| Exact Mass |
458.267
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| CAS # |
7681-14-3
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| PubChem CID |
93055
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| Appearance |
White to off-white solid powder
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| Density |
1.21 g/cm3
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| Boiling Point |
606.7ºC at 760 mmHg
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| Melting Point |
266-273°
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| Index of Refraction |
1.568
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| LogP |
3.544
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
33
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| Complexity |
925
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| Defined Atom Stereocenter Count |
7
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| SMILES |
C[C@]12C[C@@H]([C@H]3[C@H]([C@@H]1CC[C@@]2(C(=O)COC(=O)CC(C)(C)C)O)CCC4=CC(=O)C=C[C@]34C)O
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| InChi Key |
HUMXXHTVHHLNRO-KAJVQRHHSA-N
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| InChi Code |
InChI=1S/C27H38O6/c1-24(2,3)14-22(31)33-15-21(30)27(32)11-9-19-18-7-6-16-12-17(28)8-10-25(16,4)23(18)20(29)13-26(19,27)5/h8,10,12,18-20,23,29,32H,6-7,9,11,13-15H2,1-5H3/t18-,19-,20-,23+,25-,26-,27-/m0/s1
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| Chemical Name |
[2-[(8S,9S,10R,11S,13S,14S,17R)-11,17-dihydroxy-10,13-dimethyl-3-oxo-7,8,9,11,12,14,15,16-octahydro-6H-cyclopenta[a]phenanthren-17-yl]-2-oxoethyl] 3,3-dimethylbutanoate
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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 (~218.06 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.45 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (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 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.45 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 | 2.1806 mL | 10.9030 mL | 21.8060 mL | |
| 5 mM | 0.4361 mL | 2.1806 mL | 4.3612 mL | |
| 10 mM | 0.2181 mL | 1.0903 mL | 2.1806 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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