计算溶液所需的质量、体积或浓度。
| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
有货
概述
Febuxostat (非布司他; TEI 6720;TMX 67 ) 是选择性黄嘌呤氧化酶（XO）抑制剂，Ki为0.6 nM。An inhibitor xanthine oxidase and xanthine dehydrogenase
Information
Febuxostat Febuxostat (TMX 67, TEI-6720) is a selective xanthine oxidase inhibitor with K i of 0.6 nM.
In vitro
Febuxostat displays potent mixed-type inhibition of the activity of purified bovine milk xanthine oxidase, with Ki and Ki\' values of 0.6 nM and 3.1 nM respectively, indicating inhibition of both the oxidized and reduced forms of xanthine oxidase. [2]
In vivo
Febuxostat (5–6 mg/kg/day) combined with fructose significantly lowers blood pressure, UA, triglycerides, and insulin in rats compared with fructose alone. Febuxostat (5–6 mg/kg/day) combined with fructose also reduces glomerular pressure, renal vasoconstriction, and afferent arteriolar area in rats compared with fructose alone. Febuxostat prevents hyperuricemia in 5/6 nephrectomy (5/6 Nx)+oxonic acid (OA)+Febuxostat(Fx) rats and ameliorates proteinuria, preserves renal function and prevents glomerular hypertension in both 5/6 nephrectomy (5/6 Nx)+vehicle (V)+Febuxostat(Fx) and 5/6 nephrectomy (5/6 Nx)+oxonic acid (OA)+Febuxostat(Fx) groups. Febuxostat (5 mg/kg/d by gavage for 8 days) treatment after transverse aortic constriction (TAC) attenuates the TAC-induced left ventricular (LV) hypertrophy and dysfunction. Febuxostat blunts the TAC-induced increases in nitrotyrosine (indicating reduced myocardial oxidative stress), p-Erk(Thr202/Tyr204), and p-mTOR(Ser2488), with no effect on total Erk or total mTOR. Febuxostat significantly suppresses oxonic acid activity, and thereby reduces oxidative stress in Sprague-Dawley rats with right nephrectomy and left renal I/R injury, as assessed by nitrotyrosine, thiobarbituric acid-reactive substances (TBARS) and urine 8-isoprostane. Febuxostat also reduces the induction of endoplasmic reticulum (ER) stress in Sprague-Dawley rats with right nephrectomy and left renal I/R injury, as assessed by GRP-78, ATF4, and CHOP.
Cell Data
cell lines：CRC lines SW480, LoVo, DLD1 and HCT15.
Concentrations：
Incubation Time：
Powder Purity:≥99%
规格
英文别名
TMX 67, TEI-6720 | 2-(3-cyano-4-isobutoxyphenyl)-4-methylthiazole-5-carboxylic acid
规格或纯度
Moligand™, 10mM in DMSO
英文名称
Febuxostat
生化机理
非布索坦（TMX 67，TEI-6720）是一种选择性黄嘌呤氧化酶抑制剂，其Ki值为 0.6 nM。
储存条件
-80℃储存
运输条件
特低温运输
作用类型
抑制剂
作用机制
黄嘌呤脱氢酶抑制剂
名称和识别符
EC号
682-158-6
分子类型
小分子
Isomeric SMILES
CC1=C(SC(=N1)C2=CC(=C(C=C2)OCC(C)C)C#N)C(=O)O
关联CAS
NSC Number
758874
MeSH Entry Terms
2-(3-cyano-4-isobutoxyphenyl)-4-methyl-5-thiazolecarboxylic acid;6720, TEI;febuxostat;TEI 6720;TEI-6720;TEI6720;uloric
分子量
316.38
Reaxy-Rn
8005333
Reaxys-RN link address
https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=8005333&ln=
高级数据
产品属性
| ALogP | 3.9 |
|---|
关联靶点（人）
XDH
Tclin
黄嘌呤脱氢酶/氧化酶(Xanthine dehydrogenase/oxidase)
(7 活性数据)
化学和物理性质
熔点
209 °C
安全和危险性（GHS）
象形图
信号词
警告
危险声明
H413: 可能对水生生物造成长期持续有害影响
H302: 吞食有害
预防措施声明
P273: 避免释放到环境中。
P501: 将内容物/容器送到批准的废物处理厂处理
P264: 处理后要彻底洗手。
P270: 使用本产品时，请勿进食、饮水或吸烟。
P330: 漱口
P301+P317: 如果被吞咽：请寻求医疗帮助。
Merck Index
3948
质检证书(CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
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| 批号(Lot Number) | 证书类型 | 货号 |
|---|---|---|
 L2220017 |
分析证书 | F408252 |
技术文档和文章
此产品的引用文献
溶液计算器
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