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.
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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 II, IC50: 27 nM Inosine monophosphate dehydrogenase I, IC50: 39 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。 |
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]. |
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 | 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 |