Leflunomide

別名: HWA486, RS-34821, SU101 中文名稱：來(lái)氟米特

目錄號(hào)：S1247 Purity: 99.93%

Leflunomide是一種屬于DMARD的免疫抑制劑，可抑制嘧啶的合成和 protein tyrosine kinase 的活性。Leflunomide 的活性代謝產(chǎn)物為A77 1726(RS-61980)，可抑制 dihydroorotate dehydrogenase (DHODH)。Leflunomide 還是 AhR 的激動(dòng)劑。

Leflunomide Chemical Structure

CAS: 75706-12-6

規(guī)格	價(jià)格	庫(kù)存
10mM (1mL in DMSO)	1546.12	現(xiàn)貨
100mg	1190.59	現(xiàn)貨
500mg	3843.33	現(xiàn)貨
1g	5487.3	現(xiàn)貨
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產(chǎn)品質(zhì)控

批次：純度： 99.93%

99.93

Leflunomide相關(guān)產(chǎn)品

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細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

細(xì)胞系	實(shí)驗(yàn)類型	活性描述	文獻(xiàn)信息
B-cells	Function assay	In vitro inhibition of Ab formation from trinitrophenyl-lipopolysaccharide (TNP-LPS) B-cells, IC50=5.1μM	11384243
A673	qHTS assay	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	29435139
SK-N-MC	qHTS assay	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	29435139
SK-N-MC	qHTS assay	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells	29435139
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生物活性

產(chǎn)品描述

靶點(diǎn)

Dihydroorotate dehydrogenase ^[1]

體外研究(In Vitro)
體外研究活性	Leflunomide實(shí)際上是藥物前體，在體內(nèi)加工成活性代謝物A771726，這已被證明能抑制單核細(xì)胞和T細(xì)胞的增殖。Leflunomide是幾種蛋白酪氨酸激酶的抑制劑，在體外的細(xì)胞和酶測(cè)定中IC50值在30 mM和100 mM之間。^[1] Leflunomide能夠抑制抗CD3-和白細(xì)胞介素-2（IL-2）刺激的T細(xì)胞增殖。在體外酪氨酸激酶測(cè)定中，Leflunomide能夠抑制p59fyn和p56lck活性。Eflunomide也抑制Jurkat細(xì)胞中抗CD3抗體刺激的鈣動(dòng)員，而不影響ionomycin刺激的鈣動(dòng)員。Leflunomide也抑制抗CD3單克隆抗體刺激的反應(yīng)，如人T淋巴細(xì)胞中IL-2產(chǎn)生和IL-2受體表達(dá)。Leflunomide也抑制CTLL-4細(xì)胞中IL-2刺激的酪氨酸磷酸化. ^[2] Leflunomide是一種免疫調(diào)節(jié)藥物可通過(guò)抑制線粒體酶二氫乳清脫氫酶（DHODH）發(fā)揮作用，它在從頭合成的嘧啶核糖核苷酸尿苷一磷酸的過(guò)程中發(fā)揮關(guān)鍵作用。由于生產(chǎn)rUMP的不足和涉及p53的機(jī)制，Leflunomide通過(guò)細(xì)胞周期進(jìn)程的干擾防止激活與自身免疫性淋巴細(xì)胞的擴(kuò)大。^[3]
實(shí)驗(yàn)圖片	檢測(cè)方法	檢測(cè)指標(biāo)	實(shí)驗(yàn)圖片	PMID
	Western blot	CDK2 / Cyclin A2 ATF4 / CHOP DH0DH		29348830
	Growth inhibition assay	Cell viability		29423085

體內(nèi)研究(In Vivo)
體內(nèi)研究活性	在嚙齒動(dòng)物，狗，猴等中，Leflunomide能夠防止和逆轉(zhuǎn)同種異體移植物和異種移植物排斥。^[2]

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試驗(yàn)信息 (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT05605587	Recruiting	MEN1 Gene Mutation	University Hospital Basel Switzerland	May 2 2023	Not Applicable
NCT04212416	Active not recruiting	Chronic Graft Versus Host Disease\|Steroid Refractory Graft Versus Host Disease	City of Hope Medical Center\|National Cancer Institute (NCI)	May 12 2020	Phase 1
NCT04361214	Terminated	COVID-19	University of Chicago	May 5 2020	Phase 1
NCT03715699	Unknown status	Autoimmune Disease	Peking Union Medical College Hospital	July 1 2018	Not Applicable
NCT03599986	Completed	Active Rheumatoid Arthritis	Eva Pharma\|DataClin	June 16 2017	--

參考文獻(xiàn)
[1] Davis JP, et al. Biochemistry, 1996, 35(4), 1270-1273. [2] Xu X, et al. J Biol Chem. 1995, 270(21), 12398-12403. [3] Fox RI, et al. Clin Immunol, 1999, 93(3), 198-208. + 展開(kāi)

參考文獻(xiàn)

[1] Davis JP, et al. Biochemistry, 1996, 35(4), 1270-1273.
[2] Xu X, et al. J Biol Chem. 1995, 270(21), 12398-12403.
[3] Fox RI, et al. Clin Immunol, 1999, 93(3), 198-208.

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