Eniluracil是一种口服有效的二氢嘧啶脱氢酶 (DPD) 抑制剂,能够不可逆地抑制 DPD,显著提高 5-氟尿嘧啶 (5-FU) 的口服生物利用度。Eniluracil 也作为点击化学试剂,参与铜催化的叠氮-炔环加成反应 (CuAAc),适用于 5-FU 联合抗癌治疗的研究。
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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 (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 | Eniluracil, also known as 5-Ethynyluracil, is an orally active dihydropyrimidine dehydrogenase (DPD) inhibitor. Eniluracil irreversibly inhibits DPD, increases the oral bioavailability of 5-fluorouracil to 100% and promotes the homogeneous absorption and toxicity of 5-fluorouracil. Eniluracil can be used in combination with fluoropyrimidines (e.g., 5-fluorouracil) in combination for cancer research[1][2].Eniluracil contains an alkyne group that can undergo copper-catalysed azide-alkyne cycloaddition (CuAAc) with molecules containing an azide moiety, and can therefore be used as a click chemistry reagent. |
Animal study | Administered intraperitoneally at a dose of 1 mg/kg once daily for 3 days, Eniluracil greatly improves 5-fluorouracil treatment in rats[1]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
7.35mL 1.47mL 0.73mL |
36.74mL 7.35mL 3.67mL |
73.47mL 14.69mL 7.35mL |
CAS号 | 59989-18-3 |
分子式 | C6H4N2O2 |
分子量 | 136.108 |
别名 | |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Inert atmosphere,2-8°C |
溶解度 |
DMSO: 16 mg/mL(117.55 mM),配合低频超声,并水浴加热至45℃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 |