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

货号:A122692 同义名: A77 1726;Flucyamide

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.

Teriflunomide 化学结构 CAS号:163451-81-8
Teriflunomide 化学结构
CAS号:163451-81-8
Teriflunomide 3D分子结构
CAS号:163451-81-8
Teriflunomide 化学结构 CAS号:163451-81-8
Teriflunomide 3D分子结构 CAS号:163451-81-8
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Teriflunomide 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]}
批次查询: 批次纯度:

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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 ++

R132H-IDH1, IC50: 70 nM

R132C-IDH1, IC50: 0.16 μM

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 (rat), IC50: 3 nM

SCD1 (mouse), IC50: 1 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 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 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 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 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 技术信息

CAS号163451-81-8
分子式C12H9F3N2O2
分子量 270.207
别名 A77 1726;Flucyamide;SU 20;HMR-1726
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,Store in freezer, under -20°C

溶解度

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

动物实验配方
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