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.
Storage Temp
Store at -20°C
Shipped In
Ice chest + Ice pads
Grade
Moligand™
Action Type
INHIBITOR
Mechanism of action
Dihydroorotate dehydrogenase inhibitor
Product Description
Information
Vidofludimus 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 134 nM
In vitro
Vidofludimus causes a concentration dependent inhibition of phytohemagglutinin-stimulated PBMC proliferation via the inhibition of pyrimidine de novo synthesis. Vidofludimus attenuates IL-17 secretion from colonic strips by inhibition of STAT3 and NF-κB activation.
In vivo
In MRLlpr/lpr mice, Vidofludimus (300 mg/kg, p.o.) reduces systemic autoimmunity and improves Lupus Nephritis. In Rats, Vidofludimus (60 mg/kg, p.o.) effectively reduces macroscopic and histological pathology and the numbers of CD3+ T cells. In a rat model of renal transplantation, Vidofludimus (20 mg/kg, p.o.) prolongs survival, paralleled by amelioration of histologic signs of acute rejection.
1.Fitzpatrick LR, Deml L, Hofmann C, Small JS, Groeppel M, Hamm S, Lemstra S, Leban J, Ammendola A. (2010) 4SC-101, a novel immunosuppressive drug, inhibits IL-17 and attenuates colitis in two murine models of inflammatory bowel disease.. Inflamm Bowel Dis, 16 (10):(1763-77). [PMID:20310011][10.1021/op500134e]
2.Kulkarni OP, Sayyed SG, Kantner C, Ryu M, Schnurr M, Sárdy M, Leban J, Jankowsky R, Ammendola A, Doblhofer R et al.. (2010) 4SC-101, a novel small molecule dihydroorotate dehydrogenase inhibitor, suppresses systemic lupus erythematosus in MRL-(Fas)lpr mice.. Am J Pathol, 176 (6):(2840-7). [PMID:20413687][10.1021/op500134e]
3.Leban J, Vitt D. (2011) Human dihydroorotate dehydrogenase inhibitors, a novel approach for the treatment of autoimmune and inflammatory diseases.. Arzneimittelforschung, 61 (1):(66-72). [PMID:21355448][10.1021/op500134e]
4.Herrlinger KR, Diculescu M, Fellermann K, Hartmann H, Howaldt S, Nikolov R, Petrov A, Reindl W, Otte JM, Stoynov S et al.. (2013) Efficacy, safety and tolerability of vidofludimus in patients with inflammatory bowel disease: the ENTRANCE study.. J Crohns Colitis, 7 (8):(636-43). [PMID:23078909][10.1021/op500134e]
5.Muehler A, Peelen E, Kohlhof H, Gröppel M, Vitt D. (2020) Vidofludimus calcium, a next generation DHODH inhibitor for the Treatment of relapsing-remitting multiple sclerosis.. Mult Scler Relat Disord, 43 (13):(102129). [PMID:32428844][10.1021/op500134e]
6.Muehler A, Kohlhof H, Groeppel M, Vitt D. (2020) Safety, Tolerability and Pharmacokinetics of Vidofludimus calcium (IMU-838) After Single and Multiple Ascending Oral Doses in Healthy Male Subjects.. Eur J Drug Metab Pharmacokinet, 45 (5):(557-573). [PMID:32361977][10.1021/op500134e]
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G2213040