2. Metabolic Enzyme/Protease
  3. Ser/Thr Protease
  4. Benzamidine

Benzamidine is a competitive protease inhibitor that blocks the hydrolytic cleavage of glucagon by plasmin, trypsin and thrombin. Benzamidine effectively inhibits the degradation of glucagon by relevant proteases during the collection, storage and analysis of human plasma and blood samples. During in vivo metabolism, Benzamidine undergoes N-hydroxylation and produces multiple metabolites, exhibiting characteristics of delayed excretion or biphasic elimination. Benzamidine only induces slight single-strand DNA breaks at high concentrations and shows no significant genotoxic potential overall. Benzamidine may interfere with the detection of some glucagon antisera, but does not affect key antigen-antibody affinity at specific concentrations. Benzamidine can be used as a stabilizer in glucagon radioimmunoassays to ensure the accuracy and recovery rate of detection results.

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Benzamidine

Benzamidine Chemical Structure

CAS No. : 618-39-3

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 3 publication(s) in Google Scholar

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Benzamidine Related Antibodies

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  • Purity & Documentation

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Description

Benzamidine is a competitive protease inhibitor that blocks the hydrolytic cleavage of glucagon by plasmin, trypsin and thrombin. Benzamidine effectively inhibits the degradation of glucagon by relevant proteases during the collection, storage and analysis of human plasma and blood samples. During in vivo metabolism, Benzamidine undergoes N-hydroxylation and produces multiple metabolites, exhibiting characteristics of delayed excretion or biphasic elimination. Benzamidine only induces slight single-strand DNA breaks at high concentrations and shows no significant genotoxic potential overall. Benzamidine may interfere with the detection of some glucagon antisera, but does not affect key antigen-antibody affinity at specific concentrations. Benzamidine can be used as a stabilizer in glucagon radioimmunoassays to ensure the accuracy and recovery rate of detection results[1][2][3].
In Vitro

Benzamidine (0.05-0.1 M; 6-24 h at 4°C) inhibits the degradation of [125I]-glucagon in undiluted human plasma; the recovery rate of glucagon in undiluted human plasma treated with 0.05 M benzamidine exceeds 85%[1].
Benzamidine (1-20 μmoles/tube or 5-20 μmoles/tube; 1 h) exhibits only weak, marginal genotoxicity (inducing DNA single-strand breaks) in primary rat hepatocytes, and shows no genotoxicity in CO631 cells at the tested concentrations[2].
Benzamidine (1-10 μmoles/plate; 72 h) does not induce selective amplification of SV40 DNA in CO631 cells[2].

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

Benzamidine Related Antibodies

Cell Cytotoxicity Assay[2]

Cell Line: primary rat hepatocytes, CO631 cells
Concentration: 1-20 μmoles/tube or 5-20 μmoles/tube
Incubation Time: 1 h
Result: Exhibited only marginal, borderline genotoxic activity (induction of DNA single-strand breaks) in primary rat hepatocytes, and no genotoxic activity in CO631 cells at the tested concentrations
In Vivo

Benzamidine (10 mg/kg; intravenous injection; single dose) undergoes N-hydroxylation to form benzamidine oxime in male Wistar rats and grey rabbits. It is also partially excreted via urine, with benzamide detected in the urine[3].

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

Animal Model: Wistar Hannover rat (male, 200-360 g for blood sampling; 177-395 g for urine collection)[3]
Dosage: 10 mg/kg
Administration: i.v.; single dose
Result: Detected no free benzamidoxime in rat plasma or urine.
Detected benzamidoxime in rat plasma at 0.35-0.74 ng/μL after 24-hour hydrolysis with arylsulfatase.
Undetected benzamidine in rat plasma 5 hours post-administration.
Recovered 70.5 ± 29.8% of the administered dose in urine over 96 hours post-administration, with 3.3 ± 3.0% excreted on the fourth day.
Detected benzamide in rat urine samples.
Animal Model: grey (male, 4.8-5.1 kg)[3]
Dosage: 10 mg/kg
Administration: i.v.; single dose
Result: Detected no free benzamidoxime in rabbit plasma.
Detected benzamidoxime in plasma collected 30 minutes post-administration at 3.58 ± 0.31 ng/μL (equivalent to 1.79 ± 0.15 ng/μL blood) after 30-minute incubation with β-glucuronidase.
Detected benzamidoxime in plasma collected 4 hours post-administration at 3.19 ± 0.58 ng/μL after 30-minute hydrolysis with arylsulfatase.
Detected benzamidoxime in plasma collected 6 hours post-administration at 1.81 ± 0.51 ng/μL after 24-hour hydrolysis with arylsulfatase.
Observed benzamidine concentrations in rabbit plasma reached a minimum at 24 hours post-administration then increased thereafter.
Molecular Weight

120.15

Formula

C7H8N2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

N=C(C1=CC=CC=C1)N
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Store at room temperature 3 years

In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (416.15 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 8.3229 mL 41.6146 mL 83.2293 mL
5 mM 1.6646 mL 8.3229 mL 16.6459 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

  • Molarity Calculator

  • Dilution Calculator

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

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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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C2

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Volume (final)

V2

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: ≥ 5 mg/mL (41.61 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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% Corn Oil

    Solubility: ≥ 5 mg/mL (41.61 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 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 (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
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).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 95.27%

SDS (393 KB)

COA (247 KB) HNMR (245 KB) LCMS (95 KB)

Handling Instructions (2659 KB)
References

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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 8.3229 mL 41.6146 mL 83.2293 mL 208.0732 mL
5 mM 1.6646 mL 8.3229 mL 16.6459 mL 41.6146 mL
10 mM 0.8323 mL 4.1615 mL 8.3229 mL 20.8073 mL
15 mM 0.5549 mL 2.7743 mL 5.5486 mL 13.8715 mL
20 mM 0.4161 mL 2.0807 mL 4.1615 mL 10.4037 mL
25 mM 0.3329 mL 1.6646 mL 3.3292 mL 8.3229 mL
30 mM 0.2774 mL 1.3872 mL 2.7743 mL 6.9358 mL
40 mM 0.2081 mL 1.0404 mL 2.0807 mL 5.2018 mL
50 mM 0.1665 mL 0.8323 mL 1.6646 mL 4.1615 mL
60 mM 0.1387 mL 0.6936 mL 1.3872 mL 3.4679 mL
80 mM 0.1040 mL 0.5202 mL 1.0404 mL 2.6009 mL
100 mM 0.0832 mL 0.4161 mL 0.8323 mL 2.0807 mL
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Benzamidine 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:

Benzamidine618-39-3Ser/Thr ProteaseSerine proteasesSerine endopeptidasesThreonine proteasesprotease inhibitorSV40-transformed Chinese hamster embryo cellsprimary rat hepatocytesSalmonella typhimuriumthrombintrypsinglucagon degradation inhibitorCytochrome P-450 IIC3plasminhuman plasmaInhibitorinhibitorinhibit

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