Vidofludimus (Synonyms: 4sc-101; SC12267)
目录号: PL04303 纯度: ≥99%
CAS No. :717824-30-1
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中文名称
Vidofludimus
中文别名
Vidofludimus
英文名称
Vidofludimus
英文别名
1-Cyclopentene-1-carboxylic acid, 2-[[(3-fluoro-3'-methoxy[1,1'-biphenyl]-4-yl)amino]carbonyl]-;2-[[2-fluoro-4-(3-methoxyphenyl)phenyl]carbamoyl]cyclopentene-1-carboxylic acid;VidofludiMus;2-((3-fluoro-3'-methoxy-[1,1'-biphenyl]-4-yl)carbamoyl)cyclopent-1-enecarboxylic acid;2-(3-Fluoro-3'-methoxy-biphenyl-4-ylcarbamoyl)-cyclopent-1-ene-carboxylic acid;4sc-101;CHEMBL197194;KB-81442;SC12267;SureCN247888;UNII-8Y1PJ3VG81;Vidofludimus [INN];SC 12267;8Y1PJ3VG81;2-{[2-fluoro-4-(3-methoxyphenyl)phenyl]carbamoyl}cyclopent-1-ene-1-carboxylic acid;2-[[2-fluoranyl-4-(3-methoxyphenyl)phenyl]carbamoyl]cyclopentene-1-carboxylic acid;GTPL9860;BDBM16111;HMS3740I15;AOB87354;BCP14555;s726
Cas No.
717824-30-1
分子式
C20H18FNO4
分子量
355.36
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
Vidofludimus 是二氢乳清酸脱氢酶 (DHODH) 的抑制剂,也是法尼醇 X 受体 (FXR) 的新型调节剂,具有口服活性。Vidofludimus 作为一种免疫调节剂,可用于研究自身免疫性疾病,如炎症性肠病 (IBD)。Vidofludimus 还可通过靶向 FXR 用于脂肪肝的研究。
生物活性
Vidofludimus is an orally active inhibitor for dihydroorotate dehydrogenase (DHODH) and also is a novel modulator for farnesoid X receptor (FXR). Vidofludimus, as an immunomodulatory agent, can be used for the research of autoimmune disorders such as inflammatory bowel disease (IBD). Vidofludimus also can be used for the research of fatty liver by targeting FXR.
性状
Solid
IC50 & Target[1][2]
IL-17
体外研究(In Vitro)
Vidofludimus (0-1 μM) selectively activats FXR in a concentration dependent manner with an EC50 value of about 450 nM in inducing the recruitment of various coactivator LXXLL motifs.
Vidofludimus (0-8 μM) blocks nuclear translocation of p65 by suppressing IKK-IκB-NF-κB pathway.
Vidofludimus has inhibitory activity for human DHODH with an IC50 value of 160 nM.
Vidofludimus inhibits dihydro-orotate dehydrogenase and lymphocyte proliferation in vitro.
Vidofludimus inhibits interleukin (IL)-17 secretion in vitro independently of effects on lymphocyte proliferation.
Vidofludimus completely blocks IL-23 + IL-1β-stimulated secretion of IL-17 by colonic strips in ex vivo. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(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.
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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
ClinicalTrial
参考文献
[1]. Yanlin Zhu, et al. Repositioning an Immunomodulatory Drug Vidofludimus as a Farnesoid X Receptor Modulator With Therapeutic Effects on NAFLD. Front Pharmacol. 2020 May 14;11:590.
[2]. Andreas Muehler, et al. Vidofludimus calcium, a next generation DHODH inhibitor for the Treatment of relapsing-remitting multiple sclerosis. Mult Scler Relat Disord. 2020 Aug;43:102129.
溶解度数据
In Vitro: DMSO : ≥ 46 mg/mL (129.45 mM)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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