ABT (1-Aminobenzotriazole)
(Synonyms: 1-氨基苯并三唑,ABT; 3-Aminobenzotriazole) 目录号 : GC14781A non-specific CYP inhibitor
Cas No.:1614-12-6
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
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- Purity: >99.50%
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- SDS (Safety Data Sheet)
- Datasheet
Cell experiment: |
Freshly isolated human hepatocytes are used in this study. Briefly, hepatocytes are placed in serum-free Williams’ E media containing 0.1 μM dexamethasone, 10 μg/mL gentamicin, 15 mM HEPES, 2 mM L-glutamine, and 1% ITS. Cells are incubated for 10 hr at 37°C in an atmosphere containing 5% CO2. After recovery, the hepatocytes are treated with media containing CITCO (100 nM), rifampin (10 μM) or vehicle (ethanol), with or without 1-Aminobenzotriazole (ABT) (1 mM) for 72 hr[1]. |
Animal experiment: |
Male Sprague-Dawley rats (0.26 to 0.30 kg, n=3 per treatment) receive an oral dose of 1-Aminobenzotriazole (ABT) (100 mg/kg, 2 mL/kg) 2 h before a single intravenous bolus of procainamide (10 mg/kg, 2 mL/kg). The control group receives only the intravenous bolus of procainamide without 1-Aminobenzotriazole pretreatment. The vehicle for both 1-Aminobenzotriazole and procainamide is 10% dimethylacetamide/90% water (v/v). Rats are fed 4 h after dosing, and serial blood samples are collected at 0.03, 0.17, 0.25, 0.5, 1, 2, 4, and 6 h postdose. Blood samples are centrifuged using tubes containing K3-EDTA as the anticoagulant to obtain plasma. Urine samples are also collected over 24 h postdose. Plasma and urine samples are frozen at -20°C until analysis[2]. |
References: [1]. Yang K, et al. Induction of CYP2B6 and CYP3A4 expression by 1-aminobenzotriazole (ABT) in human hepatocytes. Drug Metab Lett. 2010 Aug;4(3):129-33. |
1-Aminobenzotriazole is a nonspecific and irreversible inhibitor of cytochrome P450 (P450).
1-Aminobenzotriazole (ABT) alone significantly increases the expression levels of CYP2B6 in two different hepatocytes (7.3- and 10.8-fold, respectively). Upon co-treatment with 1-Aminobenzotriazole, the induction of CYP2B6 expression by CITCO or rifampin is potentiated: 12.6- and 4.0-fold for CITCO as well as 3.9- and 2.5-fold for rifampin. 1-Aminobenzotriazole has a greater potentiation effect on CITCO than on rifampin. 1-Aminobenzotriazole alone increases the expression levels of CYP3A4 in tow different hepatocytes (by 2.0- and 3.8-fold). Upon co-treatment with 1-Aminobenzotriazole, the effects of CITCO on CYP3A4 expression levels are potentiated by 3.8- and 6.0- fold as compare to cells treated with CITCO alone[1]. 1-Aminobenzotriazole (ABT) (1 mM) shows pronounced (~95%) inhibition of the formation of N-acetylprocainamide compare with the control without 1-Aminobenzotriazole[2].
Oral 1-Aminobenzotriazole (ABT) (100 mg/kg, 2 h predose) decreases 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). The urinary recovery of procainamide increases from 18 to 30%, whereas the recovery of N-acetylprocainamide in urine decreases from 13.3 to 6.5% with 1-Aminobenzotriazole[2]. Pretreatment of rats with 100 mg/kg oral 1-Aminobenzotriazole (ABT) administered 2 hours before a semisolid caloric test meal markedly delays gastric emptying. 1-Aminobenzotriazole also increases stomach weights by 2-fold[3].
References:
[1]. Yang K, et al. Induction of CYP2B6 and CYP3A4 expression by 1-aminobenzotriazole (ABT) in human hepatocytes. Drug Metab Lett. 2010 Aug;4(3):129-33.
[2]. Sun Q, et al. 1-Aminobenzotriazole, a known cytochrome P450 inhibitor, is a substrate and inhibitor of N-acetyltransferase. Drug Metab Dispos. 2011 Sep;39(9):1674-9.
[3]. Stringer RA, et al. 1-Aminobenzotriazole modulates oral drug pharmacokinetics through cytochrome P450 inhibition and delay of gastric emptying in rats. Drug Metab Dispos. 2014 Jul;42(7):1117-24.
Cas No. | 1614-12-6 | SDF | |
别名 | 1-氨基苯并三唑,ABT; 3-Aminobenzotriazole | ||
化学名 | 1H-benzo[d][1,2,3]triazol-1-amine | ||
Canonical SMILES | NN1N=NC2=CC=CC=C12 | ||
分子式 | C6H6N4 | 分子量 | 134.14 |
溶解度 | ≥ 6.7mg/mL in DMSO | 储存条件 | Store at RT |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 7.4549 mL | 37.2745 mL | 74.549 mL |
5 mM | 1.491 mL | 7.4549 mL | 14.9098 mL |
10 mM | 0.7455 mL | 3.7274 mL | 7.4549 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
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% DMSO % % Tween 80 % saline | ||||||||||
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工作液浓度: mg/ml;
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2.
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