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(E/Z)-Teriflunomide/(E/Z)-特立氟胺 {[allProObj[0].p_purity_real_show]}

货号:A132118 同义名: (E/Z)-A77 1726

Teriflunomide, the active metabolite of an approved antirheumatic drug leflunomide, is an emerging oral therapy for multiple sclerosis (MS). It reversibly inhibits dihydroorotate dehydrogenase, the rate-limiting step in the de novo synthesis of pyrimidines.

(E/Z)-Teriflunomide/(E/Z)-特立氟胺 化学结构 CAS号:108605-62-5
(E/Z)-Teriflunomide/(E/Z)-特立氟胺 化学结构
CAS号:108605-62-5
(E/Z)-Teriflunomide/(E/Z)-特立氟胺 3D分子结构
CAS号:108605-62-5
(E/Z)-Teriflunomide/(E/Z)-特立氟胺 化学结构 CAS号:108605-62-5
(E/Z)-Teriflunomide/(E/Z)-特立氟胺 3D分子结构 CAS号:108605-62-5
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(E/Z)-Teriflunomide/(E/Z)-特立氟胺 纯度/质量文件 产品仅供科研

货号:A132118 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 Dehydrogenase 其他靶点 纯度
Trilostane 99+%
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IDH2 R140Q mutant, IC50: 23 nM

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Gimeracil 98%
AGI-5198 ++

R132C-IDH1, IC50: 0.16 μM

R132H-IDH1, IC50: 70 nM

99%+
SW033291 ++++

15-PGDH, Ki: 0.1 nM

15-PGDH, IC50: 1.5 nM

99%+
Mycophenolic acid 99+%
Fomepizole 98%
Leflunomide 98%
3-Nitropropanoic acid 99%+
Isovaleramide 99%
Mycophenolate Mofetil +++

Inosine monophosphate dehydrogenase II, IC50: 27 nM

Inosine monophosphate dehydrogenase I, IC50: 39 nM

98%
MK-8245 ++++

SCD1 (mouse), IC50: 1 nM

SCD1 (rat), IC50: 3 nM

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Vidofludimus ++

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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。

(E/Z)-Teriflunomide/(E/Z)-特立氟胺 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].

(E/Z)-Teriflunomide/(E/Z)-特立氟胺 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

(E/Z)-Teriflunomide/(E/Z)-特立氟胺 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

(E/Z)-Teriflunomide/(E/Z)-特立氟胺 技术信息

CAS号108605-62-5
分子式C12H9F3N2O2
分子量 270.21
SMILES Code C/C(O)=C(C#N)/C(NC1=CC=C(C(F)(F)F)C=C1)=O
MDL No. MFCD00910058
别名 (E/Z)-A77 1726
运输蓝冰
InChI Key UTNUDOFZCWSZMS-YFHOEESVSA-N
Pubchem ID 54684141
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Sealed in dry, room temperature

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