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Methylprednisolone sodium succinate

Alias: Methylprednisolone sodium succinate; U 9088; U-9088; U9088
Cat No.:V11390 Purity: =98.70%
Methylprednisolone sodium succinate (U-9088; 6α-Methylprednisolone 21-hemisuccinate sodium) is a water-soluble ester of Methylprednisolone(also known as NSC-19987) which is a synthetic and potent glucocorticoid receptor agonist, used to achieve prompt suppression of inflammation.
Methylprednisolone sodium succinate
Methylprednisolone sodium succinate Chemical Structure CAS No.: 2375-03-3
Product category: Bacterial
This product is for research use only, not for human use. We do not sell to patients.
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Other Forms of Methylprednisolone sodium succinate:

  • Methylprednisolone succinate
Official Supplier of:
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Purity & Quality Control Documentation

Purity: =98.70%

Product Description
Methylprednisolone sodium succinate (U-9088; 6α-Methylprednisolone 21-hemisuccinate sodium) is a water-soluble ester of Methylprednisolone (also known as NSC-19987) which is a synthetic and potent glucocorticoid receptor agonist, used to achieve prompt suppression of inflammation. It is used for cardiac, allergic, and hypoxic emergencies. Methylprednisolone sodium succinate has slightly longer half-life than that of Prednisolone.
Methylprednisolone sodium succinate (CAS 2375-03-3) is a synthetic glucocorticoid used for the treatment of various inflammatory and autoimmune conditions. It is commonly used in the treatment of asthma, rheumatoid arthritis, multiple sclerosis, and other inflammatory conditions. Methylprednisolone binds to specific nuclear receptors, alters gene expression, and reduces the production of pro-inflammatory cytokines. It also reduces the number of circulating lymphocytes and induces apoptosis in sensitive tumor cell populations.
Biological Activity I Assay Protocols (From Reference)
Targets
Methylprednisolone sodium succinate targets the glucocorticoid receptor, a nuclear receptor that regulates gene expression. By binding to this receptor, it alters the transcription of target genes, leading to anti-inflammatory and immunosuppressive effects. It reduces the production of pro-inflammatory cytokines, reduces the number of circulating lymphocytes, and induces cell differentiation and apoptosis. It is a potent anti-inflammatory agent.
ln Vitro
In vitro, methylprednisolone sodium succinate binds to the glucocorticoid receptor and modulates gene expression. It reduces the production of pro-inflammatory cytokines in immune cells. It also induces apoptosis in sensitive tumor cell populations. These activities demonstrate its potent anti-inflammatory and immunosuppressive effects.
ln Vivo
In vivo, methylprednisolone sodium succinate is used for cardiac, allergic, and hypoxic emergencies. It is used to treat conditions such as arthritis, blood disorders, severe allergic reactions, certain cancers, and eye conditions. It is a widely used corticosteroid for various inflammatory and autoimmune diseases.
Enzyme Assay
The in vitro receptor binding assay for methylprednisolone sodium succinate typically involves radioligand displacement studies using the glucocorticoid receptor. The compound's affinity for the receptor is determined by measuring its ability to displace a specific radiolabeled ligand. These cell-free assays provide a direct measure of the compound's binding affinity for the glucocorticoid receptor.
Cell Assay
In vitro cellular assays for methylprednisolone sodium succinate assess its effects on gene expression and cytokine production. Immune cells are treated with methylprednisolone, and the expression of pro-inflammatory cytokines is measured. Its effects on lymphocyte viability and apoptosis can also be assessed. These assays demonstrate the compound's functional activity in a relevant cellular context.
Animal Protocol
In vivo animal studies for methylprednisolone sodium succinate have been conducted in various animal models of inflammation and autoimmune diseases to evaluate its efficacy. However, its clinical efficacy has been established in human use for various inflammatory conditions.
ADME/Pharmacokinetics
Methylprednisolone sodium succinate is administered intravenously or intramuscularly for rapid onset of action. It is a water-soluble salt of methylprednisolone. It is metabolized in the liver and excreted in urine. It has a slightly longer half-life than prednisolone. Its pharmacokinetic properties support its use in acute and chronic conditions.
Toxicity/Toxicokinetics
Methylprednisolone sodium succinate has a well-established safety profile but is associated with significant adverse effects with long-term use. Common adverse effects include weight gain, hyperglycemia, osteoporosis, and immunosuppression. It should be used with caution in patients with diabetes, hypertension, and infections. Its safety has been established through extensive clinical use.
References

[1]. Methylprednisolone sodium succinate reduces BBB disruption and inflammation in a model mouse of intracranial haemorrhage. Brain Res Bull. 2016;127:226-233.

[2]. Li LL, Huang LL, Miu SJ, Zhang H. [Local combined with systemic glucocorticoid treatment of young and middle-aged patients with severe and profound hearing loss]. Lin Chung Er Bi Yan Hou Tou Jing Wai Ke Za Zhi. 2018 Apr;32(7):533-536. d

Additional Infomation
Methylprednisolone sodium succinate is a corticosteroid. It is the sodium salt of the synthetic glucocorticoid receptor agonist and possesses immunosuppressive and anti-inflammatory effects. In vivo, methylprednisolone sodium succinate is converted to active prednisolone, activating glucocorticoid receptor-mediated gene expression. This includes inducing the synthesis of the anti-inflammatory protein IκB-α and inhibiting the synthesis of nuclear factor κB (NF-κB). Consequently, the production of pro-inflammatory cytokines such as IL-1, IL-2, and IL-6 is downregulated, and the activation of cytotoxic T lymphocytes is suppressed. Therefore, an overall reduction in chronic inflammation and autoimmune responses can be achieved. Methylprednisolone water-soluble esters are used to treat cardiac, allergic, and hypoxic emergencies. See also: Methylprednisolone (containing the active moiety).
Methylprednisolone sodium succinate is a synthetic glucocorticoid used for the treatment of various inflammatory and autoimmune conditions. It binds to the glucocorticoid receptor, alters gene expression, and reduces pro-inflammatory cytokine production. It is commonly used in the treatment of asthma, rheumatoid arthritis, and multiple sclerosis. It is available as a prescription medication.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C26H33NAO8
Molecular Weight
496.53
Exact Mass
496.207
Elemental Analysis
C, 62.89; H, 6.70; Na, 4.63; O, 25.78
CAS #
2375-03-3
Related CAS #
Methylprednisolone succinate;2921-57-5
PubChem CID
23680530
Appearance
White to off-white solid powder
Boiling Point
689.6ºC at 760mmHg
Flash Point
230.7ºC
LogP
0.884
Hydrogen Bond Donor Count
2
Hydrogen Bond Acceptor Count
8
Rotatable Bond Count
7
Heavy Atom Count
35
Complexity
988
Defined Atom Stereocenter Count
8
SMILES
C[C@@]12[C@](C(COC(CCC([O-])=O)=O)=O)(O)CC[C@@]1([H])[C@]3([H])C[C@H](C)C4=CC(C=C[C@]4(C)[C@@]3([H])[C@@H](O)C2)=O.[Na+]
InChi Key
FQISKWAFAHGMGT-SGJOWKDISA-M
InChi Code
InChI=1S/C26H34O8.Na/c1-14-10-16-17-7-9-26(33,20(29)13-34-22(32)5-4-21(30)31)25(17,3)12-19(28)23(16)24(2)8-6-15(27)11-18(14)24/h6,8,11,14,16-17,19,23,28,33H,4-5,7,9-10,12-13H2,1-3H3,(H,30,31)/q+1/p-1/t14-,16-,17-,19-,23+,24-,25-,26-/m0./s1
Chemical Name
Pregna-1,4-diene-3,20-dione, 11-beta,17,21-trihydroxy-6-alpha-methyl-, 21- (hydrogen succinate), monosodium salt
Synonyms
Methylprednisolone sodium succinate; U 9088; U-9088; U9088
HS Tariff Code
2934.99.03.00
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Note: Please store this product in a sealed and protected environment, avoid exposure to moisture.
Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
H2O : ~50 mg/mL ~(100.70 mM)
Ethanol : ~100 mg/mL
DMSO :25~100 mg/mL (50.35~201.39 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.19 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 (4.19 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.

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Solubility in Formulation 3: ≥ 2.08 mg/mL (4.19 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
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.


Solubility in Formulation 4: 10% DMSO+40% PEG300+5% Tween-80+45% Saline: ≥ 2.08 mg/mL (4.19 mM)

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.0140 mL 10.0699 mL 20.1398 mL
5 mM 0.4028 mL 2.0140 mL 4.0280 mL
10 mM 0.2014 mL 1.0070 mL 2.0140 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.

Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

  • Calculate the Mass of a compound required to prepare a solution of known volume and concentration
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An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
  • Enter 350.26 in the Molecular Weight (MW) box
  • Enter 10 in the Concentration box and choose the correct unit (mM)
  • Enter 5 in the Volume box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
  • Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
  • Enter 25 into the Concentration (End) box and select the correct unit (mM)
  • Enter 25 into the Volume (End) box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
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  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

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  • The answer appears in the Volume (to add to vial) box
In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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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.

Clinical Trial Information
NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02425813 Withdrawn Drug: Budesonide
Drug: Methylprednisolone Sodium Succinate
Acute Graft Versus Host Disease
Intestinal Graft Versus Host Disease
Wake Forest University Health Sciences 2015-10 Phase 2
NCT05649878 Completed Drug: Evaluation of bioavailability of
methylprednisolone succinate administered intravenously
Drug: Evaluation of bioavailability of methylprednisolone
succinate administered intranasally
Healthy Subjects
Intranasal Administration
Intravenous Administration
Methylprednisone Administration
Edda Sciutto Conde 2021-11-05 Not Applicable
NCT01167946 Completed Drug: methylprednisolone sodium succinate
Drug: methylprednisolone sodium succinate
Drug: methylprednisolone sodium succinate
Alopecia Totalis
Alopecia Universalis
Ophiasic Alopecia
King Saud University 2003-01 Phase 4
NCT06360458 Recruiting Drug: Methylprednisolone sodium succinate
Drug: Placebo (Methylprednisolone sodium succinate simulant)
Acute Ischemic Stroke Wan-Jin Chen 2024-08-01 Phase 3
NCT04343729 Completed Drug: Methylprednisolone Sodium Succinate
Drug: Placebo solution
SARS-CoV Infection
Severe Acute Respiratory
Syndrome (SARS) Pneumonia
Fundação de Medicina Tropical
Dr. Heitor Vieira Dourado
2020-04-18 Phase 2
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