2. Metabolic Enzyme/Protease
  3. Ser/Thr Protease PAI-1
  4. 4-Aminobenzamidine dihydrochloride

4-Aminobenzamidine dihydrochloride  (Synonyms: p-Aminobenzamidine dihydrochloride)

Cat. No.: HY-W018723 Purity: 99.80%
SDS
COA
Handling Instructions Technical Support

4-Aminobenzamidine (p-Aminobenzamidine) dihydrochloride is a strong trypsin inhibitor. 4-Aminobenzamidine dihydrochloride acts as an orally active urokinase type plasminogen activator (uPA) inhibitor (Ki=82 μM). 4-Aminobenzamidine dihydrochloride can be used for cardiovascular diseases and anti-tumor study.

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

4-Aminobenzamidine dihydrochloride Chemical Structure

4-Aminobenzamidine dihydrochloride Chemical Structure

CAS No. : 2498-50-2

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10 mM * 1 mL in DMSO
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Customer Review

Based on 1 publication(s) in Google Scholar

4-Aminobenzamidine dihydrochloride Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE 4-Aminobenzamidine dihydrochloride

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

4-Aminobenzamidine (p-Aminobenzamidine) dihydrochloride is a strong trypsin inhibitor. 4-Aminobenzamidine dihydrochloride acts as an orally active urokinase type plasminogen activator (uPA) inhibitor (Ki=82 μM). 4-Aminobenzamidine dihydrochloride can be used for cardiovascular diseases and anti-tumor study[1][2][3][4].

IC50 & Target

Trypsin[1]
Ki: 82 μM (uPA)[1]
In Vitro

4-Aminobenzamidine dihydrochloride causes a dose-dependent inhibition of uPA activity in DU145 cells[2].
4-Aminobenzamidine dihydrochloride has an anti-proliferative effect in DU145 cells. 4-Aminobenzamidine (100-250 μM, 24 h) abolishes rat hepatocyte proliferation induced by plasminogen and EGF[2][3].
4-Aminobenzamidine (1-100 μM) dihydrochloride induces a dose-dependent vasodilator effect in intact endothelium aortic rings from Wistar and SHR[4].
4-Aminobenzamidine (1 nM) dihydrochloride evokes coronary vasodilation in the isolated hearts of Wistar rats and SHR[4].

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

4-Aminobenzamidine dihydrochloride Related Antibodies
In Vivo

4-Aminobenzamidine (250 mg/kg; p.o.; 23 days) dihydrochloride shows a clear decrease in tumor-growth rate in DU145 xenograft mice[2].
4-Aminobenzamidine (0.01-10 μg/kg; i.v.; 5-min interval between each dose injection. 1mg/kg; p.o.; daily for 60 days) dihydrochloride prevents the progress of hypertension, improved endothelial function, and attenuated the cardiac remodeling in hypertensive rats[4].

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

Animal Model: Normotensive (Wistar) and spontaneously hypertensive (SHR) male rats (180-220 g and 11-12 weeks old)[4]
Dosage: 1 mg/kg
Administration: Oral gavage (p.o.); daily for 60 days
Result: Restored the endothelium-dependent vasorelaxation in the aorta from hypertensive rats.
Ameliorated sodium nitroprusside (SNP)-induced impaired relaxation in aortic rings from SHR.
Significantly attenuated the increase of systolic blood pressure (SBP) and improved the aorta vasorelaxation induced by acetylcholine and bradykinin-induced coronary vasodilation.
Reduced the cardiomyocyte diameter in SHR heart.
Significantly reduced the interstitial collagen content in the left ventricular tissue of SHR and attenuated the perivascular fibrosis area.
Animal Model: Spontaneously hypertensive (SHR) male rats (16-20 weeks old)[4]
Dosage: 0.01, 0.1, 1, and 10 μg/kg (in 0.1 mL)
Administration: Intravenous injection (i.v.); 5-min interval between each dose injection
Result: Reduced mean arterial pressure (MAP) and increased both aortic (AVC) and mesenteric vascular conductance (MVC) in SHR.
Molecular Weight

208.09

Formula

C7H11Cl2N3
CAS No.
Appearance

Solid

Color

Off-white to light brown

SMILES

N=C(N)C1=CC=C(N)C=C1.[H]Cl.[H]Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (120.14 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 4.8056 mL 24.0278 mL 48.0557 mL
5 mM 0.9611 mL 4.8056 mL 9.6111 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
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: ≥ 1 mg/mL (4.81 mM); Clear solution

    This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 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% (20% SBE-β-CD in Saline)

    Solubility: 1 mg/mL (4.81 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 1 mg/mL.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 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.
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).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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: 99.94%

SDS (393 KB)

COA (248 KB) HNMR (254 KB) LCMS (94 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 4.8056 mL 24.0278 mL 48.0557 mL 120.1392 mL
5 mM 0.9611 mL 4.8056 mL 9.6111 mL 24.0278 mL
10 mM 0.4806 mL 2.4028 mL 4.8056 mL 12.0139 mL
15 mM 0.3204 mL 1.6019 mL 3.2037 mL 8.0093 mL
20 mM 0.2403 mL 1.2014 mL 2.4028 mL 6.0070 mL
25 mM 0.1922 mL 0.9611 mL 1.9222 mL 4.8056 mL
30 mM 0.1602 mL 0.8009 mL 1.6019 mL 4.0046 mL
40 mM 0.1201 mL 0.6007 mL 1.2014 mL 3.0035 mL
50 mM 0.0961 mL 0.4806 mL 0.9611 mL 2.4028 mL
60 mM 0.0801 mL 0.4005 mL 0.8009 mL 2.0023 mL
80 mM 0.0601 mL 0.3003 mL 0.6007 mL 1.5017 mL
100 mM 0.0481 mL 0.2403 mL 0.4806 mL 1.2014 mL
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4-Aminobenzamidine dihydrochloride 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:

4-Aminobenzamidine2498-50-2p-AminobenzamidineSer/Thr ProteasePAI-1Serine proteasesSerine endopeptidasesThreonine proteasesPlasminogen activator inhibitor-1TrypsintumorSCID miceDU145cardiovascularanti-proliferationInhibitorinhibitorinhibit

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