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

Name: 1-Aminobenzotriazole
Brand: MedChemExpress
SKU: HY-103389
Rating: 5.0 (4 reviews)

Cat. No.: HY-103389 Purity: 99.88%: FAQs
Data Sheet SDS COA Handling Instructions

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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

CAS No. : 1614-12-6

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Customer Review

Based on 4 publication(s) in Google Scholar

4 Publications Citing Use of MCE 1-Aminobenzotriazole

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•Related Screening Libraries:

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View All Cytochrome P450 Isoform Specific Products:

View All Isoforms

CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP1A2 CYP2D6 CYP2C9 CYP2C19 CYP3A4 CYP17A1

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

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

IC₅₀ & Target

CYP2

CYP3

Cellular Effect

Cell Line	Type	Value	Description	References
HepG2	IC₅₀	12 μM Compound: ABT	Inhibition of CYP4Z1 (unknown origin) in human HepG2 cell membranes transduced with lentiviral vector using luciferin-benzyl ether as substrate preincubated with NADPH for 30 mins followed by substrate addition and measured after 10 mins by P450-glo lucif Inhibition of CYP4Z1 (unknown origin) in human HepG2 cell membranes transduced with lentiviral vector using luciferin-benzyl ether as substrate preincubated with NADPH for 30 mins followed by substrate addition and measured after 10 mins by P450-glo lucif	[PMID: 32302132]
HepG2	IC₅₀	154 μM Compound: ABT	Inhibition of CYP4Z1 (unknown origin) in human HepG2 cell membranes transduced with lentiviral vector using luciferin-benzyl ether as substrate incubated for 5 mins followed by NADPH addition and measured after 20 mins by P450-glo luciferase based lumines Inhibition of CYP4Z1 (unknown origin) in human HepG2 cell membranes transduced with lentiviral vector using luciferin-benzyl ether as substrate incubated for 5 mins followed by NADPH addition and measured after 20 mins by P450-glo luciferase based lumines	[PMID: 32302132]

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].

MedChemExpress (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].

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

Molecular Weight

134.14

Formula

C₆H₆N₄

CAS No.

1614-12-6

Appearance

Solid

Color

White to light brown

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; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 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

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 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

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (15.51 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: PBS
Solubility: 25 mg/mL (186.37 mM); Clear solution; Need ultrasonic and warming and heat to 60°C

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).

Purity & Documentation

Purity: 99.88%

Select Batch:

Data Sheet (282 KB) SDS (393 KB)

COA (251 KB) HNMR (179 KB) LCMS (346 KB)

Handling Instructions (2659 KB)

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. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

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	[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. [Content Brief] [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. [Content Brief] [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. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

H₂O / DMSO	1 mM	7.4549 mL	37.2745 mL	74.5490 mL	186.3724 mL
	5 mM	1.4910 mL	7.4549 mL	14.9098 mL	37.2745 mL
	10 mM	0.7455 mL	3.7274 mL	7.4549 mL	18.6372 mL
	15 mM	0.4970 mL	2.4850 mL	4.9699 mL	12.4248 mL
	20 mM	0.3727 mL	1.8637 mL	3.7274 mL	9.3186 mL
	25 mM	0.2982 mL	1.4910 mL	2.9820 mL	7.4549 mL
	30 mM	0.2485 mL	1.2425 mL	2.4850 mL	6.2124 mL
	40 mM	0.1864 mL	0.9319 mL	1.8637 mL	4.6593 mL
	50 mM	0.1491 mL	0.7455 mL	1.4910 mL	3.7274 mL
	60 mM	0.1242 mL	0.6212 mL	1.2425 mL	3.1062 mL
	80 mM	0.0932 mL	0.4659 mL	0.9319 mL	2.3297 mL
	100 mM	0.0745 mL	0.3727 mL	0.7455 mL	1.8637 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

1-Aminobenzotriazole Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

1-Aminobenzotriazole1614-12-6ABT 3-AminobenzotriazoleCytochrome P450CYPsInhibitorinhibitorinhibit

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

Customer Review

1-Aminobenzotriazole Related Antibodies

4 Publications Citing Use of MCE 1-Aminobenzotriazole

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Cytochrome P450 Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

1-Aminobenzotriazole Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

1-Aminobenzotriazole Related Classifications

Keywords:

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