|3-(呋喃-2-基甲基)-1,8-二甲基-1H-嘌呤-2,6(3H,7H)-二酮|CsnPharm

CAS No.: 80288-49-9

Furafylline/呋拉茶碱 Catalog No. CSN22095

Synonyms: 呋拉茶碱;呋喃茶碱

Furafylline is a potent and selective inhibitor of human cytochrome P450IA2 with IC50 of 0.07 μM.

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技术信息

生物活性

描述Cytochrome P450 comprises a superfamily of structurally and functionally related isoenzymes which are involved in the metabolism of a diverse range of both exogenous and endogenous compounds. Furafylline is a potent, non-competitive inhibitor of high affinity phenacetin O-deethylase activity of microsomal fractions of human liver, a reaction catalysed by P450IA2, with an IC₅₀ value of 0.07 µM. Furafylline is a highly selective inhibitor of P450IA2 in man. Furafylline is also a potent inhibitor of the N3-demethylation of caffeine and of a component of the N1- and N7-demethylation suggesting that caffeine is a selective substrate of a hydrocarbon-inducible isoenzyme of P450 in man. Furafylline is a methylxanthine derivative that is introduced as a long-acting replacement for theophylline in the treatment of asthma. Administration of furafylline was associated with an elevation in plasma levels of caffeine, due to inhibition of caffeine oxidation, a reaction catalysed by one or more hydrocarbon-inducible isoenzymes of P450^[1].
参考文献

[1] Sesardic D, Boobis AR, Murray BP, et al. Furafylline is a potent and selective inhibitor of cytochrome P450IA2 in man. Br J Clin Pharmacol. 1990;29(6):651‐663

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.8425 mL
- 19.2124 mL
- 38.4248 mL
- 5 mM
- 0.7685 mL
- 3.8425 mL
- 7.6850 mL
- 10 mM
- 0.3842 mL
- 1.9212 mL
- 3.8425 mL

技术信息

CAS号

80288-49-9

储存条件

粉末: Keep in dark place,Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C12H12N4O3

运输

蓝冰

分子量

260.25

别名

呋拉茶碱;呋喃茶碱

溶解度

DMSO	12.0 mg/mL (46.1 mM) warming
Water	Insoluble

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