Art. -Nr.: HY-128483

Fusaric acid

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Fusaric acid is an orally active multi-pathway inhibitor with the activity of inducing oxidative stress and apoptosis. Fusaric acid can chelate divalent metal cations, damage mitochondrial membrane structure, and activate apoptosis-related proteases such as Caspase-3/7, -8, and -9. Fusaric acid also regulates Bax/Bcl-2 protein, inhibits fibrosis-related signaling pathways such as NF-κB, TGF-β₁/SMADs, and PI3K/AKT/mTOR, and reduces collagen deposition. Fusaric acid is also a dopamine β-hydroxylase inhibitor, which reduces endogenous levels of norepinephrine and epinephrine in the brain, heart, spleen, and adrenal glands. Fusaric acid can play a role in myocardial fibrosis and improve cardiac hypertrophy in heart disease, and can also be used in the study of esophageal cancer and liver cancer.

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Reinheit: 99.94%
CAS. Nr.: 536-69-6
Formel: C₁₀H₁₃NO₂
Molecular Weight:179.22

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Fusaric acid Chemical Structure

CAS. Nr.: 536-69-6

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Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Alle TGF-beta/Smad Isoform-spezifische Produkte anzeigen :

Smad1
Smad3

Alle Akt Isoform-spezifische Produkte anzeigen :

Alle mTOR Isoform-spezifische Produkte anzeigen :

Alle NF-κB Isoform-spezifische Produkte anzeigen :

Alle PI3K Isoform-spezifische Produkte anzeigen :

Alle Adrenergic Receptor Isoform-spezifische Produkte anzeigen :

In Vitro

Fusaric acid (0-500 μg/mL; 24 h) inhibits cell viability in a dose-dependent manner in human esophageal cancer cells (SNO) with an IC₅₀ value of 78.81 μg/mL^[1].
Fusaric acid (100 μM; 24-72 h) induces programmed cell death in tobacco suspension cells, accompanied by H₂O₂ accumulation, decreases mitochondrial membrane potential, and activation of caspase-3-like proteases^[2].
Fusaric acid (0-160 μM; 24-96 h) inhibits the cell viability of rat cardiomyocytes (H9C2) and mouse cardiac fibroblasts (mCFs), and suppresses the expression of fibrosis-related proteins (α-SMA, type I/III collagen) in WB results at 24 h, and downregulates TGF-β₁/SMADs and PI3K/AKT signaling pathways^[3].

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

Cell Viability Assay^[1]

Cell Line:

Cardiomyocytes isolated from mice, Rat cardiomyocytes (H9C2) and Mouse cardiac fibroblasts (mCFs)
Concentration:

1.25 μM, 2.5 μM, 5 μM, 10 μM, 20 μM, 40 μM, 80 μM, 160 μM
Incubation Time:

6 h, 12 h, 24 h, 36 h, 48 h, 72 h, 96 h
Result:

Only at the high concentration of 80 and 160 uM for long time (72 and 96 h), significant difference in cells, indicating a relatively low doses for time under 96 h showed no obvious cytotoxicity to cardiomyocytes isolated from mice and H9C2 cells.

In Vivo

Fusaric acid (50, 100 mg/kg; gavage; once a day; pretreatment for 7 days + continuous for 7 days) reduces myocardial fibrosis in the Isoprenaline (HY-B0468)-induced cardiac hypertrophy model in mice, reduces the heart weight/body weight ratio and heart weight/tibia length ratio, improves left ventricular function, and inhibits TGF-β1/SMADs and PI3K/AKT signaling pathways^[3].

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

Animal Model:

Male C57BL/6 mice (18-22 g, 8 weeks old) with Isoprenaline (HY-B0468)-induced cardiac hypertrophy and fibrosis^[3]
Dosage:

50 mg/kg, 100 mg/kg
Administration:

Oral gavage daily for 7 days before Isoprenaline treatment, then continued for another 7 days (total 15 days)
Result:

Cardiac hypertrophy markers:
Reduced heart weight/body weight and heart weight/tibia length ratios compared to the Isoprenaline group, indicating attenuated cardiac hypertrophy.
Histological analysis:
Masson's trichrome staining showed decreased collagen deposition in heart tissues, with reduced fibrosis area compared to the Isoprenaline group. WGA staining revealed smaller cardiomyocyte cross-sectional area, indicating attenuated myocyte hypertrophy.
Echocardiography:
Improved left ventricular function, including increased fractional shortening (FS%) and reduced left ventricular end-diastolic/systolic dimensions, compared to the Isoprenaline group.

Chemical Information

CAS. Nr. 536-69-6
Appearance Solid
Molecular Weight 179.22
Formel C₁₀H₁₃NO₂
Color White to off-white
SMILES

O=C(C1=NC=C(CCCC)C=C1)O
Structure Classification
- Ketones, Aldehydes, Acids
Initial Source
- Microorganisms
Fusarium spp.
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 58.33 mg/mL (325.47 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 50 mg/mL (278.99 mM; Need ultrasonic)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

5.5797 mL

27.8987 mL

55.7973 mL

5 mM

1.1159 mL

5.5797 mL

11.1595 mL

10 mM

0.5580 mL

2.7899 mL

5.5797 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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 (11.61 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.

Protocol 2

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

Solubility: ≥ 2.08 mg/mL (11.61 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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (11.61 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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Working solution concentration: 0.22 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) .

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Devnarain N, et al. Fusaric acid induces oxidative stress and apoptosis in human cancerous oesophageal SNO cells. Toxicon. 2017 Feb;126:4-11. [Content Brief]

[2]. Jiao J, et al. Hydrogen peroxide production and mitochondrial dysfunction contribute to the fusaric acid-induced programmed cell death in tobacco cells. J Plant Physiol. 2014 Aug 15;171(13):1197-203. [Content Brief]

[3]. Li X, et al. Fusaric acid (FA) protects heart failure induced by isoproterenol (ISP) in mice through fibrosis prevention via TGF-β1/SMADs and PI3K/AKT signaling pathways. Biomed Pharmacother. 2017 Sep;93:130-145. [Content Brief]

[4]. Nagatsu T, et al. Inhibition of dopamine beta-hydroxylase by fusaric acid (5-butylpicolinic acid) in vitro and in vivo. Biochem Pharmacol. 1970 Jan;19(1):35-44. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
H₂O / DMSO	1 mM	5.5797 mL	27.8987 mL	55.7973 mL	139.4934 mL
	5 mM	1.1159 mL	5.5797 mL	11.1595 mL	27.8987 mL
	10 mM	0.5580 mL	2.7899 mL	5.5797 mL	13.9493 mL
	15 mM	0.3720 mL	1.8599 mL	3.7198 mL	9.2996 mL
	20 mM	0.2790 mL	1.3949 mL	2.7899 mL	6.9747 mL
	25 mM	0.2232 mL	1.1159 mL	2.2319 mL	5.5797 mL
	30 mM	0.1860 mL	0.9300 mL	1.8599 mL	4.6498 mL
	40 mM	0.1395 mL	0.6975 mL	1.3949 mL	3.4873 mL
	50 mM	0.1116 mL	0.5580 mL	1.1159 mL	2.7899 mL
	60 mM	0.0930 mL	0.4650 mL	0.9300 mL	2.3249 mL
	80 mM	0.0697 mL	0.3487 mL	0.6975 mL	1.7437 mL
	100 mM	0.0558 mL	0.2790 mL	0.5580 mL	1.3949 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.

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Fusaric acid

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