Home Metabolism Dehydrogenase inhibitor - COVID-19 inhibitor Vidofludimus

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Vidofludimus Dehydrogenase inhibitor

Cat.No.S7262

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

Chemical Structure

Molecular Weight: 355.36

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Quality Control

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

Chemical Information, Storage & Stability

Molecular Weight 355.36 Formula

C20H18FNO4

 Storage (From the date of receipt)
CAS No. 717824-30-1 Download SDF Storage of Stock Solutions

Synonyms SC12267, 4SC-101 Smiles COC1=CC=CC(=C1)C2=CC(=C(C=C2)NC(=O)C3=C(CCC3)C(=O)O)F

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (281.4 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 1 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Mechanism of Action

Targets/IC50/Ki
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] This compound 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 this compound. 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 MRLlpr/lpr mice, Vidofludimus (300 mg/kg, p.o.) reduces systemic autoimmunity and improves Lupus Nephritis. [1] In Rats, this compound (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, this chemical (20 mg/kg, p.o.) prolongs survival, paralleled by amelioration of histologic signs of acute rejection. [3]
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00820365 Completed
Inflammatory Bowel Disease (IBD)
4SC AG
 March 2009 Phase 2

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