Vidofludimus

Catalog No.S7262 Batch:S726201

Technical Data

Formula

C₂₀H₁₈FNO₄

Molecular Weight

355.36

CAS No.

717824-30-1

Solubility (25°C)*

In vitro

DMSO

100 mg/mL (281.4 mM)

Ethanol

1 mg/mL (2.81 mM)

Water

Insoluble

In vivo (Add solvents to the product individually and in order)

Clear solution

5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O

5.0mg/ml

Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween-80 to the above system, mix evenly to clarify it; then Continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description

Vidofludimus (SC12267, 4SC-101) is an orally active and potent dihydroorotate dehydrogenase (DHODH) inhibitor with IC50 of 134 nM for human DHODH. Vidofludimus calcium (IMU-838) is investigated as a potential treatment option for COVID-19. Phase 2.

Targets

Human DHODH ^[1]

134 nM

In vitro

Vidofludimus causes a concentration dependent inhibition of phytohemagglutinin-stimulated PBMC proliferation via the inhibition of pyrimidine de novo synthesis. ^[1] Vidofludimus attenuates IL-17 secretion from colonic strips by inhibition of STAT3 and NF-κB activation. ^[2]

In vivo

In MRL^lpr/lpr mice, Vidofludimus (300 mg/kg, p.o.) reduces systemic autoimmunity and improves Lupus Nephritis. ^[1] In Rats, Vidofludimus (60 mg/kg, p.o.) effectively reduces macroscopic and histological pathology and the numbers of CD3+ T cells. ^[2] In a rat model of renal transplantation, Vidofludimus (20 mg/kg, p.o.) prolongs survival, paralleled by amelioration of histologic signs of acute rejection. ^[3]

Protocol (from reference)

Kinase Assay:^{^[1]}	DHODH inhibition assay In vitro DHODH inhibition assay mixture contains 50 μM decycloubiquinone, 100 μM dihydroorotate, and 60 μM 2,6-dichloroindophenol. The amount of enzyme is adjusted such that an average slope of approximately 0.2 AU/min will be achieved in the assay for the positive control (eg, without inhibitor). Measurements are conducted in 50 mM TrisHCl, 150 mM KCl, 0.1% Triton X-100, and pH 8.0 at 30°C in a final volume of 1 ml. The components are mixed, and the reaction is started by adding dihydroorotate. The reaction is followed spectrophotometrically by measuring the decrease in absorption at 600 nm for 2 minutes. The assay is linear in time and enzyme concentration. Inhibitory studies are conducted in a standard assay with additional variable amounts of inhibitor. For the determination of the IC50 values (concentration of inhibitor required for 50% inhibition), eight different inhibitor concentrations are applied. Each data point is recorded in triplicates on a single measurement day.
Animal Study:^{^[1]}	Animal Models MRL^lpr/lpr mice Dosages 300 mg/kg/day Administration p.o.

Kinase Assay:^{^[1]}

DHODH inhibition assay
In vitro DHODH inhibition assay mixture contains 50 μM decycloubiquinone, 100 μM dihydroorotate, and 60 μM 2,6-dichloroindophenol. The amount of enzyme is adjusted such that an average slope of approximately 0.2 AU/min will be achieved in the assay for the positive control (eg, without inhibitor). Measurements are conducted in 50 mM TrisHCl, 150 mM KCl, 0.1% Triton X-100, and pH 8.0 at 30°C in a final volume of 1 ml. The components are mixed, and the reaction is started by adding dihydroorotate. The reaction is followed spectrophotometrically by measuring the decrease in absorption at 600 nm for 2 minutes. The assay is linear in time and enzyme concentration. Inhibitory studies are conducted in a standard assay with additional variable amounts of inhibitor. For the determination of the IC50 values (concentration of inhibitor required for 50% inhibition), eight different inhibitor concentrations are applied. Each data point is recorded in triplicates on a single measurement day.

Animal Study:^{^[1]}

Animal Models
MRL^lpr/lpr mice
Dosages
300 mg/kg/day
Administration
p.o.

References

Selleck's Vidofludimus has been cited by 3 publications

Hydrogel-Based Pre-Clinical Evaluation of Repurposed FDA-Approved Drugs for AML [ Int J Mol Sci, 2023, 24(4)4235]	PubMed: 36835644
Identification of clinical candidates against West Nile Virus by activity screening in vitro and effect evaluation in vivo [ J Med Virol, 2022, 10.1002/jmv.27891]	PubMed: 35644833
Cerpegin-derived furo[3,4-c]pyridine-3,4(1H,5H)-diones enhance cellular response to interferons by de novo pyrimidine biosynthesis inhibition. [ Eur J Med Chem, 2019, 10.1016/j.ejmech.2019.111855]	PubMed: 31740051

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.