Size | Price | Stock | Qty |
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50mg |
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100mg |
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250mg |
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500mg |
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1g |
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2g |
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Other Sizes |
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Purity: ≥98%
Methylprednisolone (formerly NSC-19987; U-7532; NSC19987) is a synthetic glucocorticoid receptor agonist approved for use in the treatment of arthritis and bronchial inflammation or acute bronchitis. It is also used in the treatment of acute periods and long-term management of autoimmune diseases, most notably systemic lupus erythematosus.
Targets |
Glucocorticoid Receptor
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ln Vitro |
The main reason methylprednisolone is utilized is because it reduces inflammation. Common applications include the short-term management of bronchial inflammation or acute bronchitis brought on by a variety of respiratory conditions, as well as arthritis treatments. Methylprednisolone is used to treat autoimmune illnesses, most notably systemic lupus erythematosus, both acutely and over the long term. Vestibular neuritis is also treated with it [1]. After six months, there was a significant improvement in motor function (neurologic change scores of 16.0 and 11.2, respectively; P = 0.03), sensation to pinprick (change scores of 11.4 and 6.6; P = 0.02), and touch (change scores, 8.9 and 4.3; P = 0.03) for the patients treated with methylprednisolone within eight hours of their injury as compared to those given a placebo. both in individuals whose injuries were first assessed as neurologically complete and in individuals who were thought to have incomplete lesions [2].
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ln Vivo |
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Cell Assay |
Human immortalized gastric epithelium GES-1 and human monocyte THP-1 were cultured in RPMI-1640 containing 10% FBS and 1% penicillin-streptomycin and incubated at 37°C in a humidified incubator at 5% CO2. THP-1 cells were induced in RPMI-1640 with 100 ng/mL phorbol 12-myristate 13-acetate (PMA) for 24 h for macrophage (M0), and then was further incubated for another 24 h with 20 ng/mL IFN-γ and 10 ng/mL lipopolysaccharide (LPS) for the activation of macrophages (M1)[3].
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Animal Protocol |
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References |
[1]. Strupp, M., et al., Methylprednisolone, valacyclovir, or the combination for vestibular neuritis. N Engl J Med, 2004. 351(4): p. 354-61.
[2]. Bracken, M.B., et al., A randomized, controlled trial of methylprednisolone or naloxone in the treatment of acute spinal-cord injury. Results of the Second National Acute Spinal Cord Injury Study. N Engl J Med, 1990. 322(20): p. 1405-11. [3]. Zhen Xiang, et al. Glucocorticoids improve severe or critical COVID-19 by activating ACE2 and reducing IL-6 levels. Int J Biol Sci 2020; 16(13):2382-2391. |
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Additional Infomation |
6alpha-methylprednisolone is the 6alpha-stereoisomer of 6-methylprednisolone. It has a role as an anti-inflammatory drug, a neuroprotective agent, an antiemetic, an adrenergic agent, a xenobiotic and an environmental contaminant. It is a 6-methylprednisolone, a primary alpha-hydroxy ketone and a tertiary alpha-hydroxy ketone.
Methylprednisolone is a [prednisolone] derivative glucocorticoid with higher potency than [prednisone]. It was first described in the literature in the late 1950s. Methylprednisolone was granted FDA approval on 24 October 1957. In the outbreak of COVID-19, low dose methylprednisolone-based therapy was successful in treating COVID-19-associated pneumonia in one patient with long-term immunosuppression. The efficacy of methylprednisolone in novel coronavirus pneumonia is being investigated further in clinical trials. Methylprednisolone is a Corticosteroid. The mechanism of action of methylprednisolone is as a Corticosteroid Hormone Receptor Agonist. Methylprednisolone is a synthetic corticosteroid with anti-inflammatory and immunomodulating properties. Methylprednisolone binds to and activates specific nuclear receptors, resulting in altered gene expression and inhibition of proinflammatory cytokine production. This agent also decreases the number of circulating lymphocytes, induces cell differentiation, and stimulates apoptosis in sensitive tumor cell populations. Absorption: Oral methylprednisolone has 89.9% the bioavailability of oral methylprednisolone acetate, while rectal methylprednisolone has 14.2% the bioavailability. Intravitreal methylprednisolone has a Tmax of 2.5h. Approximately 1/10 of an oral or IV dose of methylprednisolone will reach the vitreous humor. Biological Half-Life: Methylprednisolone has a half life of 2.3h. |
Molecular Formula |
C22H30O5
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Molecular Weight |
374.47
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Exact Mass |
374.20932
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Elemental Analysis |
C, 70.56; H, 8.07; O, 21.36
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CAS # |
83-43-2
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Related CAS # |
Methylprednisolone acetate;53-36-1;Methylprednisolone (Standard);83-43-2;Methylprednisolone-d7;Methylprednisolone succinate;2921-57-5;Methylprednisolone-d3;Methylprednisolone-d4;Methylprednisolone-d2
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PubChem CID |
6741
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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 |
571.8±50.0 °C at 760 mmHg
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Melting Point |
228-237°C
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Flash Point |
313.7±26.6 °C
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Vapour Pressure |
0.0±3.6 mmHg at 25°C
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Index of Refraction |
1.603
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LogP |
1.99
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tPSA |
94.83
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SMILES |
O=C1C=C[C@]2(C)[C@@]3([H])[C@@H](O)C[C@]4(C)[C@@](O)(C(CO)=O)CC[C@@]4([H])[C@]3([H])C[ C@H](C)C2=C1
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InChi Key |
VHRSUDSXCMQTMA-PJHHCJLFSA-N
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InChi Code |
InChI=1S/C22H30O5/c1-12-8-14-15-5-7-22(27,18(26)11-23)21(15,3)10-17(25)19(14)20(2)6-4-13(24)9-16(12)20/h4,6,9,12,14-15,17,19,23,25,27H,5,7-8,10-11H2,1-3H3/t12-,14-,15-,17-,19+,20-,21-,22-/m0/s1
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Chemical Name |
(6S,8S,9S,10R,11S,13S,14S,17R)-11,17-dihydroxy-17-(2-hydroxyacetyl)-6,10,13-trimethyl-7,8,9,11,12,14,15,16-octahydro-6H-cyclopenta[a]phenanthren-3-one
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Synonyms |
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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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
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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) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.55 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 20.8 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 (5.55 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 (5.55 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 25 mg/mL (66.76 mM) in 50% PEG300 50% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication (<60°C). Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.6704 mL | 13.3522 mL | 26.7044 mL | |
5 mM | 0.5341 mL | 2.6704 mL | 5.3409 mL | |
10 mM | 0.2670 mL | 1.3352 mL | 2.6704 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.