货号:A122692
同义名:
A77 1726;Flucyamide
Teriflunomide是批准的抗风湿药物leflunomide的活性代谢物,是一种新兴的口服治疗多发性硬化症(MS)的药物。它可可逆地抑制二氢嘧啶脱氢酶,该酶是嘧啶新合成的限速步骤。
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免费溶解
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, 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。 |
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 |
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 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
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动物实验配方 |