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- 详细信息
- 文献和实验
- 技术资料
- 保存条件：
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 保质期：
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 英文名：
1-Aminobenzotriazole
- 库存：
现询
- 供应商：
北京索莱宝科技有限公司
- CAS号：
1614-12-6
- 规格：
200mg/100mg/25mg/50mg
| 规格： | 200mg | 产品价格： | ￥790.0 |
|---|---|---|---|
| 规格： | 100mg | 产品价格： | ￥590.0 |
| 规格： | 25mg | 产品价格： | ￥380.0 |
| 规格： | 50mg | 产品价格： | ￥490.0 |
| 基本信息 | |
| CAS | No.1614-12-6 |
| 中文名称 | 1-C6H7N并三唑 |
| 英文名称 | 1-Aminobenzotriazole |
| 分子式 | C6H6N4 |
| 分子量 | 134.14 |
| 溶解性 | Soluble in Water/DMSO ≥4mg/mL(Need ultrasonic) |
| 纯度 | ≥98% |
| 外观(性状) | White to light yellow Solid |
| 储存条件 | Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year |
| MDL | MFCD00132902 |
| SMILES | C1=CC=C2C(=C1)N=NN2N |
| InChIKey | JCXKHYLLVKZPKE-UHFFFAOYSA-N |
| InChI | InChI=1S/C6H6N4/c7-10-6-4-2-1-3-5(6)8-9-10/h1-4H，7H2 |
| PubChem CID | 1367 |
| 靶点 | Cytochrome P450 |
| 通路 | Metabolic Enzyme&Protease |
| 背景说明 | 1-Aminobenzotriazole 是细胞色素 P450 的非特异且不可逆抑制剂。 |
| In Vitro | 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]. |
| 细胞实验 | 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]. |
| 细胞实验 | 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]. |
| 动物实验 | 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]. |
| 数据来源文献 | [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. |
| 单位 | 瓶 |
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