Home Metabolism Dehydrogenase inhibitor - COVID-19 inhibitor Vidofludimus For research use only.

Vidofludimus

Synonyms: SC12267, 4SC-101

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.

Vidofludimus Chemical Structure

Vidofludimus Chemical Structure

CAS: 717824-30-1

Selleck's Vidofludimus has been cited by 3 publications

Purity & Quality Control

Batch: S726201 DMSO] 100 mg/mL] false] Ethanol] 1 mg/mL] false] Water] Insoluble] false Purity: 99.23%
99.23

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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
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]
Kinase Assay 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.
In Vivo
In vivo In MRLlpr/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]
Animal Research Animal Models MRLlpr/lpr mice
Dosages 300 mg/kg/day
Administration p.o.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00820365 Completed Inflammatory Bowel Disease (IBD) 4SC AG March 2009 Phase 2

Chemical lnformation & Solubility

Molecular Weight 355.36 Formula

C20H18FNO4
CAS No. 717824-30-1 SDF Download Vidofludimus SDF
Smiles COC1=CC=CC(=C1)C2=CC(=C(C=C2)NC(=O)C3=C(CCC3)C(=O)O)F
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (281.4 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 1 mg/mL

Water : Insoluble


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In vivo
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