1-Aminobenzotriazole
产品说明书
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同义名 : | ABT;3-Aminobenzotriazole;NSC 656987;NSC 114498;1-Benzotriazolylamine |
| CAS号 : | 1614-12-6 | |
| 货号 : | A336445 | |
| 分子式 : | C6H6N4 | |
| 纯度 : | 95% | |
| 分子量 : | 134.139 | |
| MDL号 : | MFCD00132902 | |
| 存储条件： |
Pure form Keep in dark place,Sealed in dry,Room Temperature In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 105 mg/mL(782.77 mM)，配合低频超声助溶，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 H2O: 50 mg/mL(372.75 mM)，配合低频超声助溶 |
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| 动物实验配方： |
| 生物活性 | |||
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| 描述 | ABT (1-Aminobenzotriazole) is a nonspecific and irreversible inhibitor of cytochrome P450 enzymes. ABT up-regulates expression of CYP2B6 and CYP3A4 potentially by activating nuclear receptor CAR. In freshly isolated human hepatocytes, ABT increased mRNA expression of CYP2B6 and CYP3A4 in a concentration-dependent manner. ABT also modulated CYP-inducing actions of CITCO and rifampin, the known inducers of CYP2B6 and CYP3A4[1]. ABT inhibit the RLS9-catalyzed N-acetylation of procainamide (IC(50) ∼ 30 μM), and no preincubation time dependence was evident. In agreement, oral ABT (100 mg/kg, 2 h predose) decreased the clearance of intravenous procainamide (45%) in rats, accompanied by a decreased N-acetylprocainamide-to-procainamide ratio in urine (0.74 versus 0.21) and plasma (area under the curve ratio 0.59 versus 0.11)[2]. The kinetic parameters of time-dependent inhibition of ABT for CYP2C9 in the absence and presence of (S)-warfarin (20 μM) were 0.0826 and 0.273 min(-1) for kinact and 3.49 and 0.157 mM for KI, respectively[3]. In vitro studies, conducted in both rat liver microsomes and rat hepatocytes, confirm that ABT is a time-dependent inhibitor of rat CYP orthologs[4]. ABT pretreatment causes long-lasting inhibition of oxidative drug metabolism without disruption of normal physiological processes[5]. | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
7.45mL 1.49mL 0.75mL |
37.27mL 7.45mL 3.73mL |
74.55mL 14.91mL 7.45mL |
| 参考文献 |
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