1. Metabolic Enzyme/Protease
  2. Cytochrome P450
  3. 1-Aminobenzotriazole

1-Aminobenzotriazole (Synonyms: ABT; 3-Aminobenzotriazole)

Cat. No.: HY-103389 Purity: 99.88%
Handling Instructions

1-Aminobenzotriazole is a nonspecific and irreversible inhibitor of cytochrome P450 (P450).

For research use only. We do not sell to patients.

1-Aminobenzotriazole Chemical Structure

1-Aminobenzotriazole Chemical Structure

CAS No. : 1614-12-6

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10 mM * 1 mL in DMSO USD 55 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

1-Aminobenzotriazole is a nonspecific and irreversible inhibitor of cytochrome P450 (P450).

IC50 & Target

P450[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

134.14

Formula

C₆H₆N₄

CAS No.
SMILES

NN1N=NC2=CC=CC=C21

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (745.49 mM; Need ultrasonic)

H2O : 50 mg/mL (372.74 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 7.4549 mL 37.2745 mL 74.5490 mL
5 mM 1.4910 mL 7.4549 mL 14.9098 mL
10 mM 0.7455 mL 3.7274 mL 7.4549 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (15.51 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (15.51 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (15.51 mM); Clear solution

  • 4.

    Add each solvent one by one:  PBS

    Solubility: 100 mg/mL (745.49 mM); Clear solution; Need ultrasonic

*All of the co-solvents are provided by MCE.
References
Cell Assay
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[2]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

Purity: 99.88%

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Keywords:

1-AminobenzotriazoleABT 3-AminobenzotriazoleCytochrome P450CYPsInhibitorinhibitorinhibit

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