| Identification | Back Directory | [Name]
VidofludiMus | [CAS]
717824-30-1 | [Synonyms]
4SC-101
CS-1196
SC12267)
VidofludiMus
VidofludiMus(4SC-101
VIDOFLUDIMUS(4SC-101; SC12267)
4SC-101; SC12267;4SC101;4SC 101
2-[(3-Fluoro-3'-methoxy-4-biphenylyl)carbamoyl]-1-cyclopentene-1-carboxylic acid
2-[[(3-Fluoro-3'-methoxy[1,1'-biphenyl]-4-yl)amino]carbonyl]-1-cyclopentene-1-carboxylic acid
1-Cyclopentene-1-carboxylic acid, 2-[[(3-fluoro-3'-methoxy[1,1'-biphenyl]-4-yl)amino]carbonyl]-
2-[(3-fluoro-3'-methoxybiphenyl-4-yl)carbamoyl]cyclopent-1-ene-1-carboxylic acid Vidofludimus(4SC-101 | [Molecular Formula]
C20H18FNO4 | [MDL Number]
MFCD18633262 | [MOL File]
717824-30-1.mol | [Molecular Weight]
355.36 |
| Chemical Properties | Back Directory | [Boiling point ]
567.5±50.0 °C(Predicted) | [density ]
1.354±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
insoluble in H2O; insoluble in EtOH; ≥103 mg/mL in DMSO | [form ]
solid | [pka]
4?+-.0.20(Predicted) | [color ]
Light yellow to gray |
| Hazard Information | Back Directory | [Uses]
Vidofludimus is an immunosuppressive drug that inhibits dihydroorotate dehydrogenase (DHODH) and the expression of proinflammatory cytokines including interleukin-17 (IL17A and IL17F) and interferon-gamma. | [Biological Activity]
vidofludimus (4sc-101, sc12267) is a novel small molecule inhibitor of dihydroorotate dehydrogenase (dhodh) with an ic50 value of 134nmol/l for human dhodh [1].vidofludimus (4sc-101, sc12267) has been reported to dose-dependently inhibit dhodh in an in vitro enzyme assay with ic50 values of 0.134μmol/l, 1.29μmol/l, 10.6μmol/l and 12.9μmol/l in human dhodh, rat dhodh, mouse dhodh and human pbmc, respectively [1]. in addition, vidofludimus has shown the inhibition of proliferation in phytohemagglutinin-induced lymphocytes with an ic50 value of ~13μmol/l. moreover, vidofludimus has been revealed to concentration-dependently inhibit phytohemagglutinin-stimulated interukin-17 secretion from human peripgeral blppd mononuclear cell lines (pbmcs) with an ic50 value of 6 μmol/l [2]. | [in vivo]
Vidofludimus (i.p.; once daily; for 14 days) exerts effects on dextran sodium sulfate (DSS) induced colitis in an FXR-dependent manner in vivo[1].
Vidofludimus (p.o; 60 mg/kg; for 6 days) effectively improves many parameters of TNBS-induced colitis in rats and has inhibitory effects on colonic STAT3 and IL-17[3]. | Animal Model: | homozygous FXR deficient (FXR KO) mice[1]
(10-week-old, male)
| | Dosage: | 20 mg/kg | | Administration: | oral, 20 mg/kg/day | | Result: | Revealed multifocal inflammatory cell infiltration and edema with crypt and epithelial cell destruction and ulceration. |
| Animal Model: | NAFLD Model[1]
(10-11 weeks old male obese Lepob/ob C57BL/6 (ob/ob) mice)
| | Dosage: | 10 mg/kg | | Administration: | intraperitoneally, once daily, for 14 days | | Result: | Significantly reduced body weight loss, prevented colonic shortening, decreased histological scores, and disease activity index (DAI) scores in WT mice.
Significantly decreased colonic mRNA expression of the pro-inflammatorygenes interleukin (IL)-1β, IL-6, IL-17, and prostaglandin-endoperoxide synthase 2 (COX-2).
|
| Animal Model: | Wistar rats[3] | | Dosage: | 60 mg/kg | | Administration: | p.o., for 6 days | | Result: | Effectively reduced macroscopic and histological pathology and the numbers of CD3+ T cells in vivo.
Reduced nuclear signal transducer and activator of transcription 3 (STAT3) binding and IL-17 levels.
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| [IC 50]
IL-17 | [References]
[1] kulkarni op1, sayyed sg, kantner c, ryu m, schnurr m, sárdy m, leban j, jankowsky r, ammendola a, doblhofer r, anders hj. 4sc-101, a novel small molecule dihydroorotate dehydrogenase inhibitor, suppresses systemic lupus erythematosus in mrl-(fas) lpr mice. am j pathol. 2010 jun;176(6):2840-7.
[2] fitzpatrick lr1, deml l, hofmann c, small js, groeppel m, hamm s, lemstra s, leban j, ammendola a. 4sc-101, a novel immunosuppressive drug, inhibits il-17 and attenuates colitis in two murine models of inflammatory bowel disease. inflamm bowel dis. 2010 oct;16(10):1763-77. |
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