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Vidofludimus

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Chemical Structure| 717824-30-1 同义名 : 4sc-101;SC12267
CAS号 : 717824-30-1
货号 : A377932
分子式 : C20H18FNO4
纯度 : 99%+
分子量 : 355.36
MDL号 : MFCD18633262
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 45 mg/mL(126.63 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

Suspended in water 21 mg/mL suspension

生物活性
靶点

  • Dehydrogenase

    Human DHODH, IC50:134 nM
描述 Vidofludimus (Vido) is a novel oral immunomodulatory drug that inhibits dihydro-orotate dehydrogenase and lymphocyte proliferation in vitro. Ex vivo Vido completely blocked IL-23 + IL-1β-stimulated secretion of IL-17 by colonic strips. In vivo Vido treatment alone most effectively reduced macroscopic and histological pathology and the numbers of CD3+ T cells[3]. Vidofludimus is 2.6 times more potent in inhibiting DHO oxidation by human DHODH (dihydroorotate dehydrogenase) compared to teriflunomide. The potency or vidofludimus to inhibit rat or mouse DHODH is 7.5 and 64.4 time lower than the for the human DHODH, respectively[4]. Moreover, vidofludimus also possesses remarkable beneficial effects in reducing NAFLD (Non-alcoholic fatty liver disease) by targeting FXR(farnesoid X receptor) [5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.81mL

0.56mL

0.28mL

14.07mL

2.81mL

1.41mL

28.14mL

5.63mL

2.81mL
参考文献

[1]Fitzpatrick LR, Small JS, et al. Vidofludimus inhibits colonic interleukin-17 and improves hapten-induced colitis in rats by a unique dual mode of action. J Pharmacol Exp Ther. 2012 Sep;342(3):850-60.

[2]Kulkarni OP, Sayyed SG, et al. 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.

[3]Fitzpatrick LR, Small JS, Doblhofer R, Ammendola A. Vidofludimus inhibits colonic interleukin-17 and improves hapten-induced colitis in rats by a unique dual mode of action. J Pharmacol Exp Ther. 2012 Sep;342(3):850-60

[4]Muehler A, Peelen E, Kohlhof H, Gröppel M, Vitt D. Vidofludimus calcium, a next generation DHODH inhibitor for the Treatment of relapsing-remitting multiple sclerosis. Mult Scler Relat Disord. 2020 Aug;43:102129

[5]Zhu Y, Xu S, Lu Y, Wei Y, Yao B, Guo F, Zheng X, Wang Y, He Y, Jin L, Li Y. Repositioning an Immunomodulatory Drug Vidofludimus as a Farnesoid X Receptor Modulator With Therapeutic Effects on NAFLD. Front Pharmacol. 2020 May 14;11:590