| Size | Price | Stock | Qty |
|---|---|---|---|
| 5g |
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| Other Sizes |
| Targets |
4-Aminobenzamidine diHCl targets serine proteases, including trypsin and urokinase-type plasminogen activator (uPA). It acts as an orally active uPA inhibitor with a Ki of 82 μM. The compound inhibits prostate tumor growth in SCID mice and can be used for cardiovascular diseases and anti-tumor studies.
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|---|---|
| ln Vitro |
In vitro, 4-Aminobenzamidine diHCl is a strong trypsin inhibitor. It acts as a relatively weak uPA inhibitor with a Ki of 82 μM. The compound shows antiplasmodial activity against Plasmodium falciparum W2 after 72 hours with an IC50 of 12589.25 nM. It inhibits prostate tumor growth in SCID mice.
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| ln Vivo |
In vivo, 4-Aminobenzamidine diHCl inhibits prostate tumor growth in SCID mice. As an orally active compound, it has potential applications in cardiovascular diseases and anti-tumor studies. However, specific in vivo efficacy data and detailed animal study results are not extensively reported in the available literature.
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| Enzyme Assay |
In vitro enzyme assays for 4-Aminobenzamidine diHCl involve protease activity assays using purified enzymes such as trypsin or uPA. The compound is incubated with the enzyme and a specific fluorogenic or chromogenic substrate. The inhibition of substrate cleavage is measured, and Ki or IC50 values are determined from dose-response curves.
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| Cell Assay |
In vitro cellular assays for 4-Aminobenzamidine diHCl are performed using cell lines to study its effects on enzyme activity and cell proliferation. Cells are treated with various concentrations of the compound, and cell viability and proliferation are assessed using standard assays. Its antiplasmodial activity is assessed using the SYBR green assay.
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| Animal Protocol |
In vivo animal studies with 4-Aminobenzamidine diHCl have been conducted in SCID mice to evaluate its effect on prostate tumor growth. The compound would be administered orally, and tumor growth inhibition would be assessed. However, specific protocols are not detailed in the available literature.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of 4-Aminobenzamidine diHCl are not extensively reported. It is known to be orally active. Specific parameters such as bioavailability, half-life, and tissue distribution are not detailed.
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| Toxicity/Toxicokinetics |
The toxicity profile of 4-Aminobenzamidine diHCl is not extensively reported. As a research compound, it is for research use only and not for human therapeutic use. No specific toxicity data are detailed.
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| References |
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| Additional Infomation |
p-Aminobenzoic acid dihydrochloride is an organic molecular entity.
4-Aminobenzamidine diHCl is a serine protease inhibitor that acts as a strong trypsin inhibitor and a weak uPA inhibitor. It inhibits prostate tumor growth in SCID mice and is used in enzyme kinetics and protein interaction studies. The compound is available for research purposes only. |
| Molecular Formula |
C7H9N3.2[HCL]
|
|---|---|
| Molecular Weight |
208.08834
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| Exact Mass |
207.033
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| CAS # |
2498-50-2
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| PubChem CID |
75626
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| Appearance |
Off-white to light brown solid powder
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| Density |
1.26g/cm3
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| Boiling Point |
289.8ºC at 760 mmHg
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| Melting Point |
>300 °C(lit.)
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| Flash Point |
129ºC
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| Vapour Pressure |
0.00216mmHg at 25°C
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| LogP |
3.538
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| Hydrogen Bond Donor Count |
5
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
12
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| Complexity |
125
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
GHEHNICLPWTXJC-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C7H9N3.2ClH/c8-6-3-1-5(2-4-6)7(9)10;;/h1-4H,8H2,(H3,9,10);2*1H
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| Chemical Name |
4-aminobenzenecarboximidamide;dihydrochloride
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~33.33 mg/mL (~160.17 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1 mg/mL (4.81 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 10.0 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 1 mg/mL (4.81 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 10.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 1 mg/mL (4.81 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.8056 mL | 24.0281 mL | 48.0561 mL | |
| 5 mM | 0.9611 mL | 4.8056 mL | 9.6112 mL | |
| 10 mM | 0.4806 mL | 2.4028 mL | 4.8056 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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