来氟米特 /Leflunomide
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货号：A133761
同义名：
SU101;HWA486
Leflunomide is a dihydroorotate dehydrogenase (DHODH) inhibitor with IC50 of 2.5 μM, it is a disease-modifying antirheumatic drug (DMARD) and inhibits de novo pyrimidine synthesis.
Leflunomide 化学结构
Leflunomide 3D分子结构
规格
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会员价
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Leflunomide 纯度/质量文件 产品仅供科研
货号：A133761
标准纯度：
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产品说明书
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Leflunomide 质控信息
Trilostane
✔
99+%
AGI-6780
+++
IDH2 R140Q mutant, IC50: 23 nM
99%+
Gimeracil
✔
98%
AGI-5198
++
R132H-IDH1, IC50: 70 nM
R132C-IDH1, IC50: 0.16 μM
99%+
SW033291
++++
15-PGDH, IC50: 1.5 nM
15-PGDH, Ki: 0.1 nM
99%+
Mycophenolic acid
✔
99+%
Fomepizole
✔
98%
Leflunomide
✔
98%
3-Nitropropanoic acid
✔
99%+
Isovaleramide
✔
98%
Mycophenolate Mofetil
+++
Inosine monophosphate dehydrogenase I, IC50: 39 nM
Inosine monophosphate dehydrogenase II, IC50: 27 nM
98%
MK-8245
++++
SCD1 (rat), IC50: 3 nM
SCD1 (mouse), IC50: 1 nM
99%+
Vidofludimus
++
Human DHODH, IC50: 134 nM
99%+
Emodin
✔
98%
Ivosidenib
✔
98%
NCT-501
++
98%
Gossypol
✔
99%+
Devimistat
✔
98%
Disulfiram
✔
98%+
Enasidenib
++++
98%
PluriSIn 1
✔
99%+
ML390
+
99%+
Teriflunomide
✔
99%+
Daidzin
+++
98+%
18β-Glycyrrhetinic acid
✔
99%
RRx-001
✔
95%
NCT-503
+
99%+
Vorasidenib
✔
99%+
Ammonium Glycyrrhizinate(x:1)
✔
98+%
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1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。
Leflunomide 生物活性
靶点
描述
Leflunomide is a low-molecular weight, synthetic, oral agent specifically developed for immunosuppression. Leflunomide reduces the clinical symptoms and signs of RA(rheumatoid arthritis), improves health related quality of life, and retards structural damage. Leflunomide has been evaluated in RA patients as monotherapy and in combination with methotrexate[3] [4] [5] [6]
Leflunomide 参考文献
[1] Davis JP, Cain GA, et al. The immunosuppressive metabolite of leflunomide is a potent inhibitor of human dihydroorotate dehydrogenase. Biochemistry. 1996 Jan 30;35(4):1270-3.
[2] Xu X, Williams JW, et al. Inhibition of protein tyrosine phosphorylation in T cells by a novel immunosuppressive agent, leflunomide. J Biol Chem. 1995 May 26;270(21):12398-403.
[3] Cannon GW, Kremer JM. Leflunomide. Rheum Dis Clin North Am. 2004 May;30(2):295-309, vi
[4] Liang C, Li J, Lu C, Xie D, Liu J, Zhong C, Wu X, Dai R, Zhang H, Guan D, Guo B, He B, Li F, He X, Zhang W, Zhang BT, Zhang G, Lu A. HIF1α inhibition facilitates Leflunomide-AHR-CRP signaling to attenuate bone erosion in CRP-aberrant rheumatoid arthritis. Nat Commun. 2019 Oct 8;10(1):4579
[5] Elshaer RE, Tawfik MK, Nosseir N, El-Ghaiesh SH, Toraih EA, Elsherbiny NM, Zaitone SA. Leflunomide-induced liver injury in mice: Involvement of TLR4 mediated activation of PI3K/mTOR/NFκB pathway. Life Sci. 2019 Oct 15;235:116824
[6] Zhang M, Qi C, Zha Y, Chen J, Luo P, Wang L, Sun Z, Wan J, Xing C, Wang S, Jiang G, Sun M, Chen Q, Chen J, Li D, Guan T, Ni Z. Leflunomide versus cyclophosphamide in the induction treatment of proliferative lupus nephritis in Chinese patients: a randomized trial. Clin Rheumatol. 2019 Mar;38(3):859-867
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Leflunomide 实验方案
计算器
摩尔计算器
总药量计算器
工作液计算器
存储液制备
1mg
5mg
10mg
1 mM
5 mM
10 mM
3.70mL
0.74mL
0.37mL
18.50mL
3.70mL
1.85mL
37.01mL
7.40mL
3.70mL
Leflunomide 技术信息
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