| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| Other Sizes |
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| Targets |
Glucocorticoid Receptor
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| ln Vitro |
Glucocorticoids remain the most widely used immunosuppressive and anti-inflammatory drugs, yet substantial gaps exist in our understanding of glucocorticoid-mediated immunoregulation. To address this, we generated a pathway-level map of the transcriptional effects of glucocorticoids on nine primary human cell types. This analysis revealed that the response to glucocorticoids is highly cell type dependent, in terms of the individual genes and pathways affected, as well as the magnitude and direction of transcriptional regulation. Based on these data and given their importance in autoimmunity, we conducted functional studies with B cells. We found that glucocorticoids impair upstream B cell receptor and Toll-like receptor 7 signaling, reduce transcriptional output from the three immunoglobulin loci, and promote significant up-regulation of the genes encoding the immunomodulatory cytokine IL-10 and the terminal-differentiation factor BLIMP-1. These findings provide new mechanistic understanding of glucocorticoid action and emphasize the multifactorial, cell-specific effects of these drugs, with potential implications for designing more selective immunoregulatory therapies[2].
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| ln Vivo |
Methylprednisolone acetate (30 mg/kg, intramuscular injection; additional oral dose of 13 mg/kg, for 10 consecutive days) combined with LPS induces the typical characteristics of early AVN of the femoral head [2].
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| Cell Assay |
Bone marrow-derived mononuclear cells were collected by incubation in hemolysis solution. Mononuclear cells were fixed in ethanol (70%) for 24 hours and stained with propidium iodide for 10 minutes. Cell cycle analysis was done by flow cytometry[2].
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| Animal Protocol |
Animal/Disease Models: Femoral necrosis mouse model methylprednisolone and lipose-induced head [2]
Doses: 30 mg/kg; 13 mg/kg for 10 days Route of Administration: 30 mg/kg, intramuscularinjection ;Additional oral dose of 13 mg/kg for 10 days resulted in chondrocyte degeneration and fibrocartilage expression after 7 weeks. The density of CD31 and VEGF-R2 markers increased in the femoral head. Adult mice were randomly divided into two groups: experimental and control. Group A (the experimental group) was given (via intramuscular injection) 10 mg/kg of lipopolysaccharide (LPS) and 30 mg/kg of methylprednisolone (MPS). Each mouse additionally received MPS in divided oral doses of 13 mg/kg for 10 consecutive days. Group B (the control group) received normal saline at the same location and same volume as those in Group A. Histological changes of the femoral heads were observed by electron microscopy at 3, 5, and 7 weeks after the last chemical injection. The percentage of empty lacunae was measured randomly and the expression of fibrocartilage was evaluated using an image analyzing system. The expression of CD31 and VEGF-R2 were observed by immunohistochemistry. The bone marrow-derived mononuclear cells were stained with propidium iodide and cell cycle was analyzed by flow cytometry.[2] |
| References |
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| Additional Infomation |
Methylprednisolone acetate is an acetate ester resulting from the formal condensation of the 21-hydroxy function of 6alpha-methylprednisolone compound with acetic acid. It has a role as an anti-inflammatory drug. It is a 20-oxo steroid, a 17alpha-hydroxy steroid, an 11beta-hydroxy steroid, a glucocorticoid, an acetate ester, a steroid ester, a 3-oxo-Delta(1),Delta(4)-steroid and a tertiary alpha-hydroxy ketone. It is functionally related to a 6alpha-methylprednisolone.
Methylprednisolone Acetate is the acetate salt of a synthetic glucocorticoid receptor agonist with immunosuppressive and antiinflammatory effects. Methylprednisolone acetate is converted into active prednisolone in the body, which activates glucocorticoid receptor mediated gene expression. This includes inducing synthesis of anti-inflammatory protein IkappaB-alpha and inhibiting synthesis of nuclear factor kappaB (NF-kappaB). As a result, proinflammatory cytokine production such as IL-1, IL-2 and IL-6 is down-regulated and cytotoxic T-lymphocyte activation is inhibited. Therefore, an overall reduction in chronic inflammation and autoimmune reactions may be achieved. Methylprednisolone derivative that is used as an anti-inflammatory agent for the treatment of ALLERGY and ALLERGIC RHINITIS; ASTHMA; and BURSITIS; and for the treatment of ADRENAL INSUFFICIENCY. See also: Methylprednisolone (has active moiety); Methylprednisolone acetate; neomycin sulfate (component of). |
| Molecular Formula |
C24H32O6
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|---|---|
| Molecular Weight |
416.50728
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| Exact Mass |
416.219
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| Elemental Analysis |
C, 69.21; H, 7.74; O, 23.05
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| CAS # |
53-36-1
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| Related CAS # |
Methylprednisolone;83-43-2
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| PubChem CID |
5877
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| Appearance |
Typically exists as white to off-white solids at room temperature
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
582.5±50.0 °C at 760 mmHg
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| Melting Point |
206ºC
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| Flash Point |
196.5±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 |
3.08
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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 |
4
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| Heavy Atom Count |
30
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| Complexity |
858
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| Defined Atom Stereocenter Count |
8
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| SMILES |
CC(OCC(C1(CCC2C3CC(C)C4=CC(C=CC4(C)C3C(CC12C)O)=O)O)=O)=O
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| InChi Key |
PLBHSZGDDKCEHR-LFYFAGGJSA-N
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| InChi Code |
InChI=1S/C24H32O6/c1-13-9-16-17-6-8-24(29,20(28)12-30-14(2)25)23(17,4)11-19(27)21(16)22(3)7-5-15(26)10-18(13)22/h5,7,10,13,16-17,19,21,27,29H,6,8-9,11-12H2,1-4H3/t13-,16-,17-,19-,21+,22-,23-,24-/m0/s1
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| Chemical Name |
2-((6S,8S,9S,10R,11S,13S,14S,17R)-11,17-dihydroxy-6,10,13-trimethyl-3-oxo-6,7,8,9,10,11,12,13,14,15,16,17-dodecahydro-3H-cyclopenta[a]phenanthren-17-yl)-2-oxoethyl acetate
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| Synonyms |
Lemod; Methylprednisolone acetate; Depo M-Predrol;Depo-Medrate Depo-medrol;Depo-Medrin Depomedrone; Depometicort Medrol Methyl prednisolone acetate; Methylprednisolone 21-acetate; NSC 48985; Medrol acetate; Mepred
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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 (~240.09 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.67 mg/mL (4.01 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 16.7 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: ≥ 1.67 mg/mL (4.01 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 16.7 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: ≥ 1.67 mg/mL (4.01 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 | 2.4009 mL | 12.0045 mL | 24.0090 mL | |
| 5 mM | 0.4802 mL | 2.4009 mL | 4.8018 mL | |
| 10 mM | 0.2401 mL | 1.2005 mL | 2.4009 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT00345046 | COMPLETEDWITH RESULTS | Drug: Pred Forte Drug: EconoPred Plus Drug: Prednisolone Acetate |
Cataract Glaucoma |
Indiana University School of Medicine | 2002-09 | Phase 4 |
| NCT01397552 | TERMINATEDWITH RESULTS | Drug: Dexamethasone Drug: methylprednisolone acetate |
Lumbar Back Pain Lumbar Radiculitis Lumbar Spine Disc Herniation |
State University of New York - Upstate Medical University | 2009-09 | Not Applicable |
| NCT00198523 | COMPLETED | Drug: Prednisolone and Tobramycin Drug: Prednisolone |
Eye Infections Postoperative Complications |
Bausch & Lomb Incorporated | 2005-07 | Phase 3 |
| NCT00699803 | COMPLETEDWITH RESULTS | Drug: T-PRED Drug: Pred Forte |
Cataract | Bausch & Lomb Incorporated | 2008-05 | Phase 2 |
| NCT00854061 | COMPLETEDWITH RESULTS | Drug: T-Pred Drug: Pred Forte |
Cataract | Bausch & Lomb Incorporated | 2009-02 | Phase 3 |
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