|1H-苯并[d] [1,2,3]三唑-1-胺|CsnPharm

CAS No.: 1614-12-6

1-氨基苯并三唑 Catalog No. CSN22313

Synonyms: ABT;3-Aminobenzotriazole;1-Benzotriazolylamine

ABT is a non-specific cytochrome P450 (CYP) inhibitor.

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实验方案

技术信息

生物活性

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].
参考文献

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
- 7.4550 mL
- 37.2749 mL
- 74.5498 mL
- 5 mM
- 1.4910 mL
- 7.4550 mL
- 14.9100 mL
- 10 mM
- 0.7455 mL
- 3.7275 mL
- 7.4550 mL

技术信息

CAS号

1614-12-6

储存条件

粉末: Keep in dark place,Sealed in dry,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C6H6N4

运输

蓝冰

分子量

134.14

别名

ABT;3-Aminobenzotriazole;1-Benzotriazolylamine;NSC 114498;NSC 656987

溶解度

DMSO	25.0 mg/mL (186.4 mM)
Water	25.0 mg/mL (186.4 mM)
Ethanol	25.0 mg/mL (186.4 mM)

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