Cat. No.: HY-N2554

Osthenol

(Synonyms: Ostenol)

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Osthenol (Ostenol) is a reversible, selective, competitive inhibitor of hMAO-A (IC₅₀=0.74 μM, K_i=0.26 μM), with antifungal and antibacterial activity. Osthenol inhibits the oxidative deamination of hMAO-A and regulates the metabolism of monoamine neurotransmitters. Osthenol also inhibits the PI3K/AKT signaling pathway to induce apoptosis of colon cancer cells, arrest the cell cycle at the G1 phase, and inhibit cell proliferation. Osthenol is mainly used in the study of neurological diseases and cancer, especially depression-related MAO-A targeted intervention and colon cancer.

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Pureté: 99.15%
CAS No.: 484-14-0
Formule: C₁₄H₁₄O₃
Masse moléculaire:230.26

Stockage:

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

Osthenol Chemical Structure

CAS No.: 484-14-0

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target^[1]

hMAO-A

0.26 μM (Ki)

hMAO-A

0.74 μM (IC₅₀)

Voir tous les produits spécifiques à Isoform Monoamine Oxidase :

MAO-A
MAO-B

Voir tous les produits spécifiques à Isoform Akt :

Voir tous les produits spécifiques à Isoform PI3K :

Cellular Effect

Cell Line	Type	Value	Description	References
Neutrophil	IC₅₀	>10 μM Compound: 16	Antiinflammatory activity in human neutrophil assessed as inhibition of FMLP/CB-induced elastase release for 5 mins Antiinflammatory activity in human neutrophil assessed as inhibition of FMLP/CB-induced elastase release for 5 mins	[PMID: 24798144]
Neutrophil	IC₅₀	2.6 μM Compound: 16	Antiinflammatory activity in human neutrophil assessed as inhibition of FMLP/CB-induced superoxide anion generation pretreated for 5 mins by spectrophotometry Antiinflammatory activity in human neutrophil assessed as inhibition of FMLP/CB-induced superoxide anion generation pretreated for 5 mins by spectrophotometry	[PMID: 24798144]
Raji	IC₅₀	290 molar ratio Compound: 9	Inhibition of TPA-induced EBV-early antigen activation in human Raji cells Inhibition of TPA-induced EBV-early antigen activation in human Raji cells	[PMID: 16441065]

In Vitro

Osthenol (0.74 μM; enzyme activity assay) exhibits potent, selective and reversible competitive inhibitory activity against recombinant hMAO-A with IC₅₀=0.74 μM, SI >81.1^[1].
Osthenol (25-100 μM; 24-48 h) significantly inhibits cell proliferation, induces apoptosis, arrests the cell cycle at the G1 phase and inhibits cell migration in HCT116 human colon cancer cells assay^[2].
Osthenol has antifungal activity with MICs of 125 μg/mL against Fusarium solani and 250 μg/mL against Candida albicans and Aspergillus fumigatus^[3].
Osthenol is effective against Gram-positive bacteria with MICs of 125-62.5 μg/mL^[4].

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

Apoptosis Analysis^[2]

Cell Line:

Apoptosis Assay (HCT116 Cells) HCT116
Concentration:

25-100 μM
Incubation Time:

48 h
Result:

Total apoptotic cells rose from 7.06% (control) to 30.12% (25 μM), 33.11% (50 μM), and 52.5% (100 μM).
Dose-dependently increased the activation of caspase-3, -8, and -9 (cleaved caspase levels increasing).

In Vivo

Osthenol (5 mg/kg; intravenous injection; single dose) has a rapid distribution characteristic in male ICR mice, with initial blood concentration C₀=14.3 μg/mL, T_1/2=47.0 min, AUC_last=211.5 μg·min/mL, MRT_last=22.5 min^[5].
Osthenol (5 mg/kg, 20 mg/kg; oral gavage; single dose) has extremely low bioavailability in male ICR mice (0.43% and 0.02%, respectively), and is rapidly metabolized to sulfonylated (M1) and glucuronidated (M2) conjugates after oral administration^[5].

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

Chemical Information

CAS No. 484-14-0
Appearance Solid
Masse moléculaire 230.26
Formule C₁₄H₁₄O₃
Color White to yellow
SMILES

O=C1C=CC2=CC=C(O)C(C/C=C(C)\C)=C2O1
Synonyms

Ostenol
Structure Classification
- Phenylpropanoids
- Coumarins
- Phenols
- Polyphenols
Initial Source
- Plants
- Umbelliferae
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

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

Solvant et solubilité

In Vitro:

DMSO : 100 mg/mL (434.29 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

4.3429 mL

21.7146 mL

43.4292 mL

5 mM

0.8686 mL

4.3429 mL

8.6858 mL

10 mM

0.4343 mL

2.1715 mL

4.3429 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.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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: 2.5 mg/mL (10.86 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.

Protocol 2

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

Solubility: ≥ 2.5 mg/mL (10.86 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (10.86 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 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.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (277 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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)
Instruction de manipulation (2659 KB)

Références

[1]. Baek SC, et al. Osthenol, a prenylated coumarin, as a monoamine oxidase A inhibitor with high selectivity. Bioorg Med Chem Lett. 2019 Mar 15;29(6):839-843. [Content Brief]

[2]. Zhuang B, et al. Osthenol inhibits the viability of HCT116 cells through suppressing PI3K/AKT signaling pathway. Int J Clin Exp Pathol, 2017, 10(6): 6308-6315.

[3]. Montagner C, et al. Antifungal activity of coumarins. Z Naturforsch C J Biosci. 2008 Jan-Feb;63(1-2):21-8. [Content Brief]

[4]. de Souza SM, et al. Antibacterial activity of coumarins. Z Naturforsch C J Biosci. 2005 Sep-Oct;60(9-10):693-700. [Content Brief]

[5]. Cho P, et al. Characterization of osthenol metabolism in vivo and its pharmacokinetics. Xenobiotica. 2020 Jul;50(7):839-846. [Content Brief]

[6]. Nemolochnova AG, et al. Stability Study, Quantification Method and Pharmacokinetics Investigation of a Coumarin-Monoterpene Conjugate Possessing Antiviral Properties against Respiratory Syncytial Virus. Pharmaceuticals (Basel). 2022 Sep 18;15(9):1158. [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
DMSO	1 mM	4.3429 mL	21.7146 mL	43.4292 mL	108.5729 mL
	5 mM	0.8686 mL	4.3429 mL	8.6858 mL	21.7146 mL
	10 mM	0.4343 mL	2.1715 mL	4.3429 mL	10.8573 mL
	15 mM	0.2895 mL	1.4476 mL	2.8953 mL	7.2382 mL
	20 mM	0.2171 mL	1.0857 mL	2.1715 mL	5.4286 mL
	25 mM	0.1737 mL	0.8686 mL	1.7372 mL	4.3429 mL
	30 mM	0.1448 mL	0.7238 mL	1.4476 mL	3.6191 mL
	40 mM	0.1086 mL	0.5429 mL	1.0857 mL	2.7143 mL
	50 mM	0.0869 mL	0.4343 mL	0.8686 mL	2.1715 mL
	60 mM	0.0724 mL	0.3619 mL	0.7238 mL	1.8095 mL
	80 mM	0.0543 mL	0.2714 mL	0.5429 mL	1.3572 mL
	100 mM	0.0434 mL	0.2171 mL	0.4343 mL	1.0857 mL

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Osthenol

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Voir tous les produits spécifiques à Isoform Monoamine Oxidase

Voir tous les produits spécifiques à Isoform Akt

Voir tous les produits spécifiques à Isoform PI3K

Activité biologique

Chemical Information