CAS NO: | 717824-30-1 |
规格: | ≥98% |
包装 | 价格(元) |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
50mg | 电议 |
100mg | 电议 |
250mg | 电议 |
500mg | 电议 |
Molecular Weight (MW) | 355.36 |
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Formula | C20H18FNO4 |
CAS No. | 717824-30-1 |
Storage | -20℃ for 3 years in powder form |
-80℃ for 2 years in solvent | |
Solubility (In vitro) | DMSO: 100 mg/mL (281.4 mM) |
Water: <1 mg/mL | |
Ethanol: <1 mg/mL | |
Solubility (In vivo) | Chemical Name: 2-((3-fluoro-3'-methoxy-[1,1'-biphenyl]-4-yl)carbamoyl)cyclopent-1-enecarboxylic acid InChi Key: XPRDUGXOWVXZLL-UHFFFAOYSA-N InChi Code: InChI=1S/C20H18FNO4/c1-26-14-5-2-4-12(10-14)13-8-9-18(17(21)11-13)22-19(23)15-6-3-7-16(15)20(24)25/h2,4-5,8-11H,3,6-7H2,1H3,(H,22,23)(H,24,25) SMILES Code: COC1=CC=CC(C2=CC(F)=C(NC(C3=C(C(O)=O)CCC3)=O)C=C2)=C1 |
Synonyms | 4SC101; SC-12267; SC12267, 4SC-101; 4SC 101; SC 12267. |
In Vitro | In vitro activity: 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. Kinase 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. Cell Assay: 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. 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. |
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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 |
Animal model | MRLlpr/lpr mice |
Formulation & Dosage | Suspended in water; 300 mg/kg; p.o. administration |
References | Am J Pathol. 2010 Jun;176(6):2840-7; J Pharmacol Exp Ther. 2012 Sep;342(3):850-60. |