Vamorolone
Based on 1 Customer Validation
Vamorolone (VBP15) is a first-in-class, orally active dissociative steroidal anti-inflammatory agent and membrane-stabilizer. Vamorolone improves muscular dystrophy without side effects. Vamorolone shows potent NF-κB inhibition and substantially reduces hormonal effects.
For research use only. We do not sell to patients.
- Purity: 99.96%
- CAS No.: 13209-41-1
- Formula: C22H28O4
- Molecular Weight:356.46
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| C2C12 | EC50 |
6.59 x 10-8 M
Compound: VBP15
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Inhibition of TNFalpha-induced NFkappaB activation in mouse C2C12 cells incubated for 24 hrs prior to TNFalpha induction measured after 24 hrs by luciferase reporter gene assay
Inhibition of TNFalpha-induced NFkappaB activation in mouse C2C12 cells incubated for 24 hrs prior to TNFalpha induction measured after 24 hrs by luciferase reporter gene assay
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[PMID: 23498916] |
| C2C12 | EC50 |
6.59 x 10-2 μM
Compound: VBP15
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Inhibition of TNFalpha-induced NFkappaB activation in mouse C2C12 cells incubated for 24 hrs prior to TNFalpha induction measured after 24 hrs by luciferase reporter gene assay
Inhibition of TNFalpha-induced NFkappaB activation in mouse C2C12 cells incubated for 24 hrs prior to TNFalpha induction measured after 24 hrs by luciferase reporter gene assay
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[PMID: 23498916] |
Vamorolone (VBP15)? inhibits TNFα-induced pro-inflammatory NF-κB signaling in C2C12 muscle cells at 1 nM or more. Vamorolone binds the glucocorticoid receptor (GR) and mineralocorticoid receptor (MR) with similar affinity[1].
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Vamorolone (0.1, 1μM; 30 minutes) reduces production of IL1βand CCL5 inflammatory mediators in primary human macrophages[2].
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Vamorolone is a first-in-class mineralocorticoid receptor (MR) antagonist/dissociative glucocorticoid receptor (GR) ligand[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
? Vamorolone (30 mg/kg; orally; daily for 20 days) reduces CNS Inflammation in murine experimental autoimmune encephalomyelitis[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 mice (experimental autoimmune encephalomyelitis)[2]
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Dosage:30 mg/kg
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Administration:Orally; daily for 20 days (starting one day prior to MOG 33-55 peptide immunization and continuing)
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Result:Reduced CNS inflammation in murine experimental autoimmune encephalomyelitis.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 13209-41-1
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Appearance Solid
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Molecular Weight 356.46
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Formula C22H28O4
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Color White to yellow
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SMILES
C[C@@]12[C@](C(CO)=O)(O)[C@H](C)C[C@@]1([H])[C@]3([H])CCC4=CC(C=C[C@]4(C)C3=CC2)=O
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Synonyms
VBP15
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 62.5 mg/mL (175.34 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (5.84 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (5.84 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (276 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Handling Instructions (2659 KB)
References
[1]. Heier CR, et al. VBP15, a novel anti-inflammatory and membrane-stabilizer, improves muscular dystrophy without side effects. EMBO Mol Med. 2013 Oct;5(10):1569-85. [Content Brief]
[2]. Dillingham BC, et al. VBP15, a novel anti-inflammatory, is effective at reducing the severity of murine experimental autoimmune encephalomyelitis. Cell Mol Neurobiol. 2015 Apr;35(3):377-387. [Content Brief]
[3]. Heier CR, et al. Vamorolone targets dual nuclear receptors to treat inflammation and dystrophic cardiomyopathy. Life Sci Alliance. 2019 Feb 11;2(1). pii: e201800186. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.8054 mL | 14.0268 mL | 28.0536 mL | 70.1341 mL |
| 5 mM | 0.5611 mL | 2.8054 mL | 5.6107 mL | 14.0268 mL | |
| 10 mM | 0.2805 mL | 1.4027 mL | 2.8054 mL | 7.0134 mL | |
| 15 mM | 0.1870 mL | 0.9351 mL | 1.8702 mL | 4.6756 mL | |
| 20 mM | 0.1403 mL | 0.7013 mL | 1.4027 mL | 3.5067 mL | |
| 25 mM | 0.1122 mL | 0.5611 mL | 1.1221 mL | 2.8054 mL | |
| 30 mM | 0.0935 mL | 0.4676 mL | 0.9351 mL | 2.3378 mL | |
| 40 mM | 0.0701 mL | 0.3507 mL | 0.7013 mL | 1.7534 mL | |
| 50 mM | 0.0561 mL | 0.2805 mL | 0.5611 mL | 1.4027 mL | |
| 60 mM | 0.0468 mL | 0.2338 mL | 0.4676 mL | 1.1689 mL | |
| 80 mM | 0.0351 mL | 0.1753 mL | 0.3507 mL | 0.8767 mL | |
| 100 mM | 0.0281 mL | 0.1403 mL | 0.2805 mL | 0.7013 mL |