Art. -Nr.: HY-109017

Vamorolone

(Synonyms: VBP15)

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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.

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Reinheit: 99.96%
CAS. Nr.: 13209-41-1
Formel: C₂₂H₂₈O₄
Molecular Weight:356.46

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Vamorolone Chemical Structure

CAS. Nr.: 13209-41-1

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Biologische Aktivität
- Beschreibung
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Alle NF-κB Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
C2C12	EC₅₀	6.59 x 10^-8 M Compound: VBP15	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	[PMID: 23498916]
C2C12	EC₅₀	6.59 x 10^-2 μM Compound: VBP15	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	[PMID: 23498916]

In Vitro

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].
? Vamorolone (0.1, 1μM; 30 minutes) reduces production of IL1βand CCL5 inflammatory mediators in primary human macrophages^[2].
? 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.

In Vivo

Vamorolone (5-30 mg/kg; cherry syrup) shows a superior side effect profile compared to pharmacological glucocorticoids in mdx mice^[1].
? 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.

Animal Model:

C57BL/6 mice (experimental autoimmune encephalomyelitis)^[2]
Dosage:

30 mg/kg
Administration:

Orally; daily for 20 days (starting one day prior to MOG 33-55 peptide immunization and continuing)
Result:

Reduced CNS inflammation in murine experimental autoimmune encephalomyelitis.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 13209-41-1
Appearance Solid
Molecular Weight 356.46
Formel C₂₂H₂₈O₄
Color White to yellow
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
Synonyms

VBP15
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.8054 mL

14.0268 mL

28.0536 mL

5 mM

0.5611 mL

2.8054 mL

5.6107 mL

10 mM

0.2805 mL

1.4027 mL

2.8054 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (5.84 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

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Vamorolone

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Alle NF-κB Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Vamorolone Related Classifications

HY-109017 Related Classifications