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.
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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, 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 (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。 |
靶点 |
|
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]. |
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 << |
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 |
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 |