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Teriflunomide/特立氟胺 {[allProObj[0].p_purity_real_show]}

货号:A122692 同义名: A77 1726; Flucyamide

Teriflunomide 是Leflunomide 的活性代谢物,可逆抑制二氢嘧啶脱氢酶,常用于多发性硬化症的研究。

Teriflunomide/特立氟胺 化学结构 CAS号:163451-81-8
Teriflunomide/特立氟胺 化学结构
CAS号:163451-81-8
Teriflunomide/特立氟胺 3D分子结构
CAS号:163451-81-8
Teriflunomide/特立氟胺 化学结构 CAS号:163451-81-8
Teriflunomide/特立氟胺 3D分子结构 CAS号:163451-81-8
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Teriflunomide/特立氟胺 纯度/质量文件 产品仅供科研

货号:A122692 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+%
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, 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 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。

Teriflunomide/特立氟胺 生物活性

靶点
  • Dehydrogenase

描述 Teriflunomide primarily inhibits dihydroorotate dehydrogenase (DHODH), crucial in pyrimidines' de novo synthesis, thereby reducing high-avidity proliferating T and B lymphocytes' activity and potentially moderating autoantigen-induced inflammation in MS, making it more cytostatic than cytotoxic towards leukocytes[1].
体内研究

Teriflunomide has shown effectiveness in two independent animal models of demyelinating disease, evidenced by its prophylactic and therapeutic benefits in both the dark agouti and female Lewis rat models of experimental autoimmune encephalitis (EAE), highlighting delayed disease onset and reduced symptom severity[1].

体外研究

Teriflunomide primarily inhibits dihydroorotate dehydrogenase (DHODH), crucial in pyrimidines' de novo synthesis, thereby reducing high-avidity proliferating T and B lymphocytes' activity and potentially moderating autoantigen-induced inflammation in MS, making it more cytostatic than cytotoxic towards leukocytes[1].

Teriflunomide/特立氟胺 细胞实验

Cell Line
Concentration Treated Time Description References
Primary rat oligodendroglial precursors 1, 5, 10 µM 24 hours To investigate the effect of Teriflunomide on oligodendroglial cell differentiation, it was found that 5 μM concentration upregulated transcript levels of myelin markers such as CNPase and PLP. J Neuroinflammation. 2018 Mar 13;15(1):76.
Primary rat oligodendroglial precursors 5 µM 24 hours To investigate the effect of Teriflunomide pulse stimulation on oligodendroglial cell differentiation, it was found that a 24-hour pulse increased CNPase protein expression. J Neuroinflammation. 2018 Mar 13;15(1):76.
U937 cells 10 and 30 µM 24 hours Reduced cytokine secretion (CXCL10, 3-fold; CCL2, 2.5-fold; IL-6, 2.2-fold; p<0.001) J Neuroinflammation. 2017 Mar 11;14(1):51.
HMC3 cells 10 and 30 µM 24 hours Reduced cytokine secretion (CXCL10, 3-fold; CCL2, 2.5-fold; IL-6, 2.2-fold; p<0.001) J Neuroinflammation. 2017 Mar 11;14(1):51.
Candida albicans 64 µg/mL 24 hours The combination of teriflunomide and fluconazole showed significant synergistic inhibitory effects on resistant Candida albicans. Front Cell Infect Microbiol. 2023 Dec 19;13:1282320.
Murine astrocytes 1, 10, 30 µM 24 hours or 72 hours To investigate the effect of teriflunomide on astrocyte metabolism, it was found that teriflunomide increased glycolytic ATP production at both 24 and 72 hours, with a significant bias toward glycolytic ATP production at 72 hours. Sci Rep. 2022 Feb 23;12(1):3049.
Oligodendrocyte precursor cells (OPCs) 10 nM to 5 µM 24, 48, and 96 hours TF decreased OPC proliferation and promoted differentiation at concentrations ranging from 10 nM to 5 μM Neurol Neuroimmunol Neuroinflamm. 2021 Oct 12;8(6):e1091.
Acute hippocampal slices 50 µM 30 minutes To investigate the effects of teriflunomide on neuronal activity and mitochondrial function under oxidative stress, results showed that teriflunomide restored tissue respiration and prevented the depression of synaptic transmission. Int J Mol Sci. 2022 Jan 28;23(3):1538.
Candida albicans 64 µg/mL 4 hours The combination of teriflunomide and fluconazole inhibited the immature biofilm formation of resistant Candida albicans. Front Cell Infect Microbiol. 2023 Dec 19;13:1282320.
Choroid plexus epithelial cells 0.1 µM to 2 mM 5 days Teriflunomide significantly reduced JCPyV infection and spread in choroid plexus epithelial cells Int J Mol Sci. 2021 Sep 10;22(18):9809.
Primary human astrocytes 0.1 µM to 2 mM 5 days Teriflunomide significantly reduced JCPyV infection and spread in primary human astrocytes Int J Mol Sci. 2021 Sep 10;22(18):9809.
Adult mouse oligodendrocyte precursor cells (OPCs) 10 nM 96 hours TF promoted differentiation of adult OPCs Neurol Neuroimmunol Neuroinflamm. 2021 Oct 12;8(6):e1091.
CD8 T cells 100 µM Teriflunomide inhibited the proliferation of CD8 T cells, and this inhibition could be reversed by the addition of uridine. Front Immunol. 2021 Oct 5;12:730342.

Teriflunomide/特立氟胺 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Xenopus laevis Mbp:GFP-NTR transgenic Xenopus laevis Administered in water 1, 10, and 100 μM For 3 days TF promoted remyelination in Xenopus laevis Neurol Neuroimmunol Neuroinflamm. 2021 Oct 12;8(6):e1091.
Galleria mellonella Galleria mellonella larvae Injection 1.6 µg/larvae Single injection, lasting 4 days The combination of teriflunomide and fluconazole significantly increased the survival rates of Galleria mellonella larvae infected with resistant Candida albicans, and reduced the fungal burden and tissue damage. Front Cell Infect Microbiol. 2023 Dec 19;13:1282320.
C57BL/6 mice Cuprizone-mediated demyelination model Oral 10 mg/kg/day Pulse administration: 7 consecutive days during the fourth week of cuprizone challenge; Continuous administration: final 18 days of cuprizone treatment Teriflunomide efficiently boosted myelin repair activities in the cuprizone-mediated demyelination model, leading to accelerated generation of oligodendrocytes and restoration of myelin sheaths. Moreover, teriflunomide restored mitochondrial integrity within oligodendroglial cells. J Neuroinflammation. 2023 Jan 7;20(1):7
Syrian Gold hamsters SARS-CoV-2 infection model Oral 10 mg/kg Twice daily for 6 days Evaluate the inhibitory effect of drug combination on SARS-CoV-2 replication, results showed combination treatment significantly reduced viral load iScience. 2022 May 20;25(5):104293.

Teriflunomide/特立氟胺 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02509052 Recurrent Plasma Cell Myeloma ... 展开 >> Refractory Plasma Cell Myeloma 收起 << Phase 1 Phase 2 Active, not recruiting June 2019 United States, California ... 展开 >> City of Hope Medical Center Duarte, California, United States, 91010 收起 <<
NCT02559765 - Completed - United Kingdom ... 展开 >> The University of Glasgow Glasgow, United Kingdom, G12 8LL 收起 <<
NCT03709446 Breast Neoplasms ... 展开 >> Breast Diseases Metastatic Triple Negative Breast Cancer 收起 << Phase 1 Phase 2 Not yet recruiting October 20, 2021 United States, New York ... 展开 >> Icahn School of Medicine at Mount Sinai Not yet recruiting New York, New York, United States, 10029 Contact: Charles Shapiro, MD    212-241-3131    charles.shapiro@mssm.edu    Contact: Joni Gomes, BSN    212-824-7076    joni.gomes@mssm.edu 收起 <<

Teriflunomide/特立氟胺 参考文献

[1]Oh J, et al. An update of teriflunomide for treatment of multiple sclerosis. Ther Clin Risk Manag. 2013;9:177-90.

Teriflunomide/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

Teriflunomide/特立氟胺 技术信息

CAS号163451-81-8
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 A77 1726; Flucyamide; SU 20; HMR-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, store in freezer, under -20°C

溶解方案

DMSO: 35 mg/mL(129.53 mM),配合低频超声助溶,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

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
方案 一
方案 二
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