产品说明书

Leflunomide

Print
Chemical Structure| 75706-12-6 同义名 : SU101;HWA486;Leflunomide, Arava, Leflunomidum, HWA-486;HW 486;Arava;RS-34821
CAS号 : 75706-12-6
货号 : A133761
分子式 : C12H9F3N2O2
纯度 : 98%
分子量 : 270.21
MDL号 : MFCD00867593
存储条件：

粉末 Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
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：
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].
实验方案
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
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