3-Methylxanthine是一种黄嘌呤衍生物和环磷酸鸟苷(GMP)抑制剂,在豚鼠分离的气管肌肉中测得其IC50值为 920 μM。
产品描述
3-Methylxanthine, a xanthine derivative, is a cyclic guanosine monophosphate (GMP) inhibitor, with an IC50 of 920 μM on guinea-pig isolated trachealis muscle.3-Methylxanthine inhibited xanthine crystallization, it could protect patients with xanthinuria from the development of renal xanthine calculi.
体外活性
To identify in vitro inhibitors of xanthine crystallization that have potential for inhibiting the formation of xanthine crystals in urine and preventing the development of the renal calculi in patients with xanthinuria. METHODS AND RESULTS: The formation of xanthine crystals in synthetic urine and the effects of 10 potential crystallization inhibitors were assessed using a kinetic turbidimetric system with a photometer. The maximum concentration tested for each compound was: 20 mg/L for 3-Methylxanthine (3-MX); 40 mg/L for 7-methylxanthine (7-MX), 1-methylxanthine (1-MX), theobromine (TB), theophylline, paraxanthine, and caffeine; 45 mg/L for 1-methyluric acid; 80 mg/L for 1,3-dimethyluric acid; and 200 mg/L for hypoxanthine. Scanning electron microscopy was used to examine the morphology of the crystals formed when inhibitory effects were observed. Only 7-MX, 3-MX, and 1-MX significantly inhibited xanthine crystallization at the tested concentrations. Mixtures of inhibitors had an additive effect rather than a synergistic effect on crystallization. CONCLUSIONS: Two of the inhibitors identified here-7-MX and 3-MX-are major metabolites of TB. In particular, after TB consumption, 20% is excreted in the urine as TB, 21.5% as 3-MX, and 36% as 7-MX. Thus, consumption of theobromine could protect patients with xanthinuria from the development of renal xanthine calculi. Clinical trials are necessary to demonstrate these effects in vivo.
Cas No.
1076-22-8
分子式
C6H6N4O2
分子量
166.14
储存和溶解度
1M NaOH:50 mg/mL (300.95 mM),ultrasonic and adjust pH to 11 with 1M NaOH
DMSO:2.61 mg/mL (15.71 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years