Leflunomide | SU101 | DHODH Inhibitor | AmBeed-信号通路专用抑制剂

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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
CAS号：75706-12-6

Leflunomide 3D分子结构
CAS号：75706-12-6

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Leflunomide 纯度/质量文件产品仅供科研

货号：A133761 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

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脱氢酶亚型比较

产品名称	Dehydrogenase ↓ ↑	纯度
Trilostane	✔	99+%
AGI-6780	+++ IDH2 R140Q mutant, IC50: 23 nM	99%+
Gimeracil	✔	98%
AGI-5198	++ R132C-IDH1, IC50: 0.16 μM R132H-IDH1, IC50: 70 nM	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 (mouse), IC50: 1 nM SCD1 (rat), IC50: 3 nM	99%+
Vidofludimus	++ Human DHODH, IC50: 134 nM	99%+
Emodin	✔	98%
Ivosidenib	✔	98%
NCT-501	++ ALDH1A1, IC50: 40 nM	98%
Gossypol	✔	99%+
Devimistat	✔	98%
Disulfiram	✔	98%+
Enasidenib	++++ IDH2, IC50: 12 nM	98%
PluriSIn 1	✔	99%+
ML390	+ DHODH, IC50: 0.56 μM	99%+
Teriflunomide	✔	99%+
Daidzin	+++ ALDH-Ⅰ, Ki: 20 nM	98+%
18β-Glycyrrhetinic acid	✔	99%
RRx-001	✔	95%
NCT-503	+ PHGDH, IC50: 2.5 μM	99%+
Vorasidenib	✔	99%+
Ammonium Glycyrrhizinate(x:1)	✔	98+%
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

Dehydrogenase

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]. Leflunomide itself induces AHR-ARNT interaction to inhibit hepatic CRP production and attenuate bone erosion in CRPL (CRPLower, CRPL) arthritic rats^[4]. A significant elevation of liver enzymes in leflunomide-treated mice (10 mg/kg) and histopathological examination revealed higher necro-inflammatory scores in leflunomide-treated mice. Furthermore, leflunomide-treated mice (5 or 10 mg/kg) showed greater staining for NFκB compared to vehicle control^[5]. Compared with cyclophosphamide, low-dose leflunomide in combination with prednisone showed both effectiveness and safety in the induction therapy of proliferative lupus nephritis in Chinese patients^[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

Leflunomide 实验方案

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

CAS号	75706-12-6
分子式	C₁₂H₉F₃N₂O₂
分子量	270.21

别名	SU101;HWA486;Leflunomide, Arava, Leflunomidum, HWA-486;HW 486;Arava;RS-34821
运输	蓝冰

存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,Room Temperature

溶解度

DMSO: 50 mg/mL(185.04 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

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全球学术期刊中引用的产品

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最近浏览的产品

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