(E/Z)-Teriflunomide

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Chemical Structure| 108605-62-5 同义名 : (E/Z)-A77 1726
CAS号 : 108605-62-5
货号 : A132118
分子式 : C12H9F3N2O2
纯度 : 99+%
分子量 : 270.21
MDL号 : MFCD00910058
存储条件:

Pure form Sealed in dry, room temperature

In solvent -20°C:3-6个月-80°C:12个月

溶解度 : -
动物实验配方:
生物活性
描述 Teriflunomide (Random Configuration) is a disease-modifying immunomodulatory drug with anti-inflammatory properties that selectively and reversibly inhibits the mitochondrial enzyme dihydro-orotate dehydrogenase, with consequent inhibition of de novo pyrimidine synthesis and reduced lymphocyte proliferation. Oral teriflunomide is an effective and generally well tolerated treatment in patients with relapsing multiple sclerosis (MS)[3]. Effects on time to failure were comparable between teriflunomide and IFNβ-1a. There was no difference between teriflunomide (14 mg) and IFNβ-1a on ARR (annualised relapse rate), though ARR was higher with teriflunomide (7 mg)[4]. Low teriflunomide concentrations resulted in cell cycle exit while higher doses led to decreased cell survival. Short-term teriflunomide pulses can efficiently promote oligodendroglial cell differentiation suggesting that young, immature cells could benefit from such stimulation. In vitro myelination can be boosted by means of an early stimulation window with teriflunomide[5].
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]Oh J, O'Connor PW. An update of teriflunomide for treatment of multiple sclerosis. Ther Clin Risk Manag. 2013;9:177-90.

[2]Hail N Jr, Chen P, et al. Evidence supporting a role for dihydroorotate dehydrogenase, bioenergetics, and p53 in selective teriflunomide-induced apoptosis in transformed versus normal human keratinocytes. Apoptosis. 2012 Mar;17(3):258-68.

[3]Scott LJ. Teriflunomide: A Review in Relapsing-Remitting Multiple Sclerosis. Drugs. 2019 Jun;79(8):875-886

[4]Vermersch P, Czlonkowska A, Grimaldi LM, Confavreux C, Comi G, Kappos L, Olsson TP, Benamor M, Bauer D, Truffinet P, Church M, Miller AE, Wolinsky JS, Freedman MS, O'Connor P; TENERE Trial Group. Teriflunomide versus subcutaneous interferon beta-1a in patients with relapsing multiple sclerosis: a randomised, controlled phase 3 trial. Mult Scler. 2014 May;20(6):705-16

[5]Göttle P, Manousi A, Kremer D, Reiche L, Hartung HP, Küry P. Teriflunomide promotes oligodendroglial differentiation and myelination. J Neuroinflammation. 2018 Mar 13;15(1):76