| Size | Price | Stock | Qty |
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| 500mg |
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| 1g |
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| Targets |
The primary target of Prednisone acetate is the glucocorticoid receptor (GR), a nuclear receptor that regulates gene transcription. Upon binding to GR, the compound induces a conformational change in the receptor, leading to its translocation into the nucleus, where it binds to glucocorticoid response elements (GREs) in the DNA and modulates the transcription of target genes. This results in the upregulation of anti-inflammatory proteins (e.g., lipocortin-1, IL-10) and the downregulation of pro-inflammatory genes (e.g., cytokines, chemokines, adhesion molecules). Additionally, Prednisone acetate has been described as a Notch inhibitor, suggesting that it may also modulate Notch signaling pathways. Its anti-inflammatory activity and ability to enhance immune responses are mediated through these mechanisms.
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| ln Vitro |
Prednisone acetate is a potent anti-inflammatory and immunomodulatory agent. It binds to the glucocorticoid receptor with high affinity and exerts its effects by modulating gene expression. It has been shown to inhibit the production of pro-inflammatory cytokines, suppress immune cell activation, and reduce inflammation. In vitro, it is commonly used to study glucocorticoid signaling and the regulation of inflammatory responses. Its physicochemical properties include a molecular weight of 400.47 g/mol, a LogP of 2.66, and a melting point of 240-242°C. It is a white to off-white solid powder with a purity of ≥98%.
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| ln Vivo |
Prednisone acetate (5 mg/kg, gavage, once daily, for 4 weeks) leads to neuronal damage in the hippocampus's dentate gyrus, which lowers glutamate (Glu) and NMDAR2A. This degrades the hippocampal LTP injury model mice. memory [1]. In patients with experimental autoimmune uveitis (EAU), prednisone acetate (6 mg/kg, gavage, once day for 15 days) improves peripheral regulatory responses in the eyes by regulating Notch signaling gain.
In vivo, Prednisone acetate is an orally active glucocorticoid that exerts potent anti-inflammatory and immunosuppressive effects. It has been studied in various animal models. In a study on C57BL/6 mice, oral administration of 5 mg/kg of Prednisone acetate once daily for 4 weeks led to neuronal damage in the hippocampus's dentate gyrus and caused memory impairment. In a model of experimental autoimmune uveitis (EAU), administration of 6 mg/kg of Prednisone acetate once daily for 15 days improved peripheral regulatory responses in the eyes by modulating Notch signaling. These studies demonstrate the compound's potent in vivo activity and its effects on the immune system and the central nervous system. |
| Enzyme Assay |
In vitro receptor binding assays for Prednisone acetate can be performed using the glucocorticoid receptor. In a typical assay, the compound is incubated with a radiolabeled glucocorticoid (e.g., [³H]-dexamethasone) and a preparation of the glucocorticoid receptor (e.g., from a cell lysate or purified protein). The amount of bound radioligand is measured, and the IC₅₀ is calculated. Alternatively, a reporter gene assay can be used, where cells are transfected with a glucocorticoid-responsive reporter gene and treated with the compound. The activity of the reporter gene (e.g., luciferase) is measured, and the EC₅₀ is determined. These assays provide a measure of the compound's affinity and activity at the glucocorticoid receptor.
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| Cell Assay |
In vitro cell-based assays for Prednisone acetate are used to study its effects on immune cells and inflammatory responses. A common assay involves treating immune cells (e.g., macrophages, T cells) with the compound and measuring the production of pro-inflammatory cytokines (e.g., TNF-α, IL-6, IL-1β) by ELISA or multiplex assays. The compound's ability to inhibit cytokine production is a measure of its anti-inflammatory activity. Cell viability assays (e.g., MTT) can be performed to assess its effects on cell proliferation and survival. The compound's effects on Notch signaling can be studied by measuring the expression of Notch target genes (e.g., Hes1) by qPCR.
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| Animal Protocol |
Animal/Disease Models: C57BL/6 mice[1]
Doses: 5 mg/kg Route of Administration: gavage (ig) Experimental Results:Body weight obviously failed to increase. Population peak value (%) diminished after high-frequency stimulation. The number of crossovers was diminished compared to the control group. It leads to memory impairment and creates a tendency for more severe impairment. Reduces glutamate and gamma-aminobutyric acid (GABA) levels in the hippocampus. diminished hippocampal N-methyl-D-aspartate receptor expression. Animal/Disease Models: Experimental autoimmune uveitis [2] Doses: 6 mg/kg Route of Administration: gavage Experimental Results: Symptoms in the eyes were diminished from the 9th day after immunization. diminished inflammation in EAU rats. Binds to pockets of Notch signaling-related molecules with good affinity. Exhibits anti-inflammatory effects by inhibiting Notch signaling activation. The frequencies of Th1 and Th17 diminished and the frequencies of Th2 and Treg increased in EAU. In vivo animal studies for Prednisone acetate are conducted in models of inflammation, autoimmune diseases, and other conditions. In the experimental autoimmune uveitis (EAU) model, mice are immunized with a retinal antigen, and the compound is administered orally. Clinical scores of eye inflammation are assessed, and the frequencies of Th1, Th17, Th2, and Treg cells are measured by flow cytometry. In the hippocampal LTP injury model, mice are treated with the compound, and cognitive function is assessed using behavioral tests. These studies provide critical data on the compound's in vivo efficacy and its mechanism of action. |
| ADME/Pharmacokinetics |
Prednisone acetate is an orally active glucocorticoid with a molecular weight of 400.47 g/mol and a LogP of 2.66. It is rapidly absorbed after oral administration and is converted to prednisone, the active form of the drug. It is metabolized in the liver and excreted in the urine. The compound has a half-life of approximately 2-4 hours. For research purposes, it is soluble in DMSO and can be formulated for oral administration. It is stable as a powder at -20°C for up to three years. Its pharmacokinetic properties are well-characterized due to its clinical use.
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| Toxicity/Toxicokinetics |
The toxicological profile of Prednisone acetate is well-established due to its clinical use as a corticosteroid. Common side effects include weight gain, increased appetite, mood changes, insomnia, and fluid retention. Long-term use can lead to more serious side effects, such as osteoporosis, diabetes, hypertension, immunosuppression, and Cushing's syndrome. It is contraindicated in patients with systemic fungal infections and should be used with caution in patients with diabetes, hypertension, or peptic ulcer disease. For laboratory handling, standard safety precautions for research chemicals should be observed. The compound is intended for research use only and is not for human therapeutic or diagnostic use.
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| References |
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| Additional Infomation |
Cetirizine is a steroid ester, 20-oxosteroid, acetate, 17α-hydroxysteroid, 11-oxosteroid, 3-oxo-Δ(1),Δ(4)steroid and tertiary α-hydroxy ketone. It is functionally associated with prednisone.
Prednisone acetate is a synthetic glucocorticoid and the acetate ester of prednisone. It is an orally bioavailable glucocorticoid receptor agonist with anti-inflammatory and immunomodulating properties. It has also been described as an orally bioavailable Notch inhibitor. The compound has a molecular formula of C₂₃H₂₈O₆ and a molecular weight of approximately 400.47 g/mol. It is supplied as a white to off-white solid powder with a purity of ≥98%. Prednisone acetate is for research use only. |
| Molecular Formula |
C23H28O6
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|---|---|
| Molecular Weight |
400.47
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| Exact Mass |
400.188
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| CAS # |
125-10-0
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| Related CAS # |
Prednisone;53-03-2;Prednisone acetate-d3
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| PubChem CID |
91438
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| Appearance |
White to off-white solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
582.0±50.0 °C at 760 mmHg
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| Melting Point |
240-242°C (dec.)
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| Flash Point |
200.2±23.6 °C
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| Vapour Pressure |
0.0±3.7 mmHg at 25°C
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| Index of Refraction |
1.580
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| LogP |
2.66
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
29
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| Complexity |
869
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| Defined Atom Stereocenter Count |
6
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| SMILES |
CC(=O)OCC(=O)[C@]1(CC[C@@H]2[C@@]1(CC(=O)[C@H]3[C@H]2CCC4=CC(=O)C=C[C@]34C)C)O
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| InChi Key |
MOVRKLZUVNCBIP-RFZYENFJSA-N
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| InChi Code |
InChI=1S/C23H28O6/c1-13(24)29-12-19(27)23(28)9-7-17-16-5-4-14-10-15(25)6-8-21(14,2)20(16)18(26)11-22(17,23)3/h6,8,10,16-17,20,28H,4-5,7,9,11-12H2,1-3H3/t16-,17-,20+,21-,22-,23-/m0/s1
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| Chemical Name |
[2-[(8S,9S,10R,13S,14S,17R)-17-hydroxy-10,13-dimethyl-3,11-dioxo-6,7,8,9,12,14,15,16-octahydrocyclopenta[a]phenanthren-17-yl]-2-oxoethyl] 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) |
DMSO : ~25 mg/mL (~62.43 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.24 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% 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 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: ≥ 2.08 mg/mL (5.19 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 20.8 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. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (5.19 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4971 mL | 12.4853 mL | 24.9707 mL | |
| 5 mM | 0.4994 mL | 2.4971 mL | 4.9941 mL | |
| 10 mM | 0.2497 mL | 1.2485 mL | 2.4971 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.
Androgen Deprivation Therapy Combined With Docetaxel for High Risk Prostate Cancer
CTID: NCT04869371
Phase: Phase 2 Status: Unknown status
Date: 2022-12-29
Products are for research use only; We do not sell to patients
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