Leflunomide

別名: HWA486, RS-34821, SU101 中文名稱：來氟米特

目錄號：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 的激動劑。

Leflunomide Chemical Structure

CAS: 75706-12-6

規(guī)格	價格	庫存
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
更大包裝有超大折扣
400-668-6834 [email protected]

產(chǎn)品質(zhì)控

批次：純度： 99.93%

99.93

Leflunomide相關產(chǎn)品

相關靶點	ALDH1A	點擊展開
相關產(chǎn)品	Glycyrrhizin (NSC 167409) Devimistat (CPI-613) Gossypol Acetate Emodin AGI-5198 AGI-6780 Sodium Dichloroacetate (DCA) NCT-503 Brequinar SW033291 RRx-001 Gossypol Farudodstat Vidofludimus Vorasidenib (AG-881) Orludodstat (BAY 2402234) Merimepodib BVT 2733 NCT-501 Enoxolone Gimeracil ML390 Alpha-Mangostin Alda 1 BAY 1436032 GSK 2837808A AG-120 (racemic) G6PDi-1 Brequinar Sodium	點擊展開
相關化合物庫	代謝化合物庫抗癌代謝化合物庫谷氨酰胺代謝化合物庫糖代謝化合物庫脂代謝化合物庫	點擊展開

細胞實驗數(shù)據(jù)示例

細胞系	實驗類型	活性描述	文獻信息(PMID)
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
點擊查看更多細胞系數(shù)據(jù)

生物活性

產(chǎn)品描述

靶點

Dihydroorotate dehydrogenase ^[1]

體外研究(In Vitro)
體外研究活性	Leflunomide實際上是藥物前體，在體內(nèi)加工成活性代謝物A771726，這已被證明能抑制單核細胞和T細胞的增殖。Leflunomide是幾種蛋白酪氨酸激酶的抑制劑，在體外的細胞和酶測定中IC50值在30 mM和100 mM之間。^[1] Leflunomide能夠抑制抗CD3-和白細胞介素-2（IL-2）刺激的T細胞增殖。在體外酪氨酸激酶測定中，Leflunomide能夠抑制p59fyn和p56lck活性。Eflunomide也抑制Jurkat細胞中抗CD3抗體刺激的鈣動員，而不影響ionomycin刺激的鈣動員。Leflunomide也抑制抗CD3單克隆抗體刺激的反應，如人T淋巴細胞中IL-2產(chǎn)生和IL-2受體表達。Leflunomide也抑制CTLL-4細胞中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程中發(fā)揮關鍵作用。由于生產(chǎn)rUMP的不足和涉及p53的機制，Leflunomide通過細胞周期進程的干擾防止激活與自身免疫性淋巴細胞的擴大。^[3]
實驗圖片	檢測方法	檢測指標	實驗圖片	PMID
	Growth inhibition assay	Cell viability		29423085
	Western blot	DH0DH ATF4 / CHOP CDK2 / Cyclin A2		23977077

體內(nèi)研究(In Vivo)
體內(nèi)研究活性	在嚙齒動物，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
https://pubmed.ncbi.nlm.nih.gov/8573583/ https://pubmed.ncbi.nlm.nih.gov/7759480/ https://pubmed.ncbi.nlm.nih.gov/10600330/ https://pubmed.ncbi.nlm.nih.gov/16904479/ + 展開

參考文獻

https://pubmed.ncbi.nlm.nih.gov/8573583/
https://pubmed.ncbi.nlm.nih.gov/7759480/
https://pubmed.ncbi.nlm.nih.gov/10600330/

https://pubmed.ncbi.nlm.nih.gov/16904479/

+ 展開