Yakuchinone B
Based on 1 Customer Validation
Yakuchinone B is an orally active and potent 5-LOX and COX-1/2 inhibitor with IC50 values of 0.37, 53.9, and 42 μM, respectively, and can be isolated and extracted from Alpinia oxyphylla. Yakuchinone B exhibits anti-inflammatory, antioxidant, and antitumor activities. Yakuchinone B exerts anti-inflammatory protective effects by inhibiting 5-LOX/COX activity and AP-1 DNA binding, downregulating the expression of pro-inflammatory factors, and modulating the gut microbiota metabolic axis to promote short-chain fatty acid production. Yakuchinone B can be used for research on colitis and cancer.
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- Pureté : 99.58%
- CAS No.: 81840-57-5
- Formule: C20H22O3
- Masse moléculaire:310.39
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Stockage:
-20°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
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5-LOX 0.37 μM (IC50) |
Ovine COX-1 53.9 μM (IC50) |
Ovine COX-2 42 μM (IC50) |
TNF-α |
In Vitro
Yakuchinone B (50-100 µM; pretreatment for 30 min, co-treatment for 12 h) inhibits TNF-α production in TPA (HY-18739)-stimulated HL-60 cells[4].
Yakuchinone B (10-100 μM; 10 min pretreatment, 30 min TPA stimulation) attenuates TPA-induced superoxide anion production in differentiated HL-60 cells[4].
Yakuchinone B (0.5-10 μM; 20 min) inhibits lipid peroxidation in rat brain homogenates[4].
Yakuchinone B (0.01-100 μM; 15 min) inhibits 5-LOX activity in RBL-1 cell lysate supernatant with an IC50 of 0.37 µM[2].
Yakuchinone B (0.01-100 μM; preincubation for 10 min followed by co-incubation with 0.5 µM A23187 for 10 min) inhibits A23187 (HY-N6687)-induced production of LTB4 and LTC4 in RBL-1 cells, with IC50 values of 0.49 µM and 0.61 µM, respectively[2].
Yakuchinone B inhibits COX-1 and COX-2 activity in sheep seminal vesicle microsomes and the activity of sheep placental COX-2 preparations, with IC50 values of 53.9 µM and 42.0 µM, respectively[2].
Yakuchinone B (1-100 μM; pre-incubation for 2 h; co-incubation for 6 h) inhibits the adhesion of U937 monocytes and EoL-1 eosinophils to TNF-α (HY-P7058)-treated HUVECs[3].
Yakuchinone B (1-100 μM; pretreatment for 2 h, co-treatment with TNF-α or IL-1β for 6 h or 8 h) inhibits the expression of the cell surface adhesion molecules E-selectin, VCAM-1, and ICAM-1 in TNF-α- or IL-1β (HY-P78459)-treated HUVECs[3].
Yakuchinone B (100 μM; pretreatment for 30 min, TPA stimulation for 1 h) inhibits transcription factor AP-1 binding to DNA (AP-1 activation) in NIH3T3 cells[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:TNF-α- or IL-1β-treated human umbilical vein endothelial cells (HUVEC)
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Concentration:1, 10, 30, 50, 100 μM
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Incubation Time:pre-treated for 2 h, co-treated with TNF-α or IL-1β for 6 hours or 8 h
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Result:Significantly suppressed the TNF-α- or IL-1β-induced cell surface expression of E-selectin, VCAM-1, and ICAM-1 in endothelial cells
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Cell Line:human promyelocytic leukemia HL-60 cells
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Concentration:50, 100 µM
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Incubation Time:pre-treated for 30 min, followed by 12 h of treatment
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Result:Significantly inhibited the massive production of TNF-α stimulated by TPA.
In Vivo
Yakuchinone B (50 μmol; t.d.; single administration; 5.5 h) inhibits epidermal ornithine decarboxylase (ODC) activity in a TPA-induced epidermal ornithine decarboxylase activation ICR mouse model[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CD-1 (male)[6]
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Dosage:100 mg/kg, 200 mg/kg
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Administration:i.g.; once daily; days 7-21
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Result:Significantly attenuated DSS-induced body weight loss, elevated disease activity index (DAI), colonic shortening, and splenomegaly.
Ameliorated histopathological mucosal damage in the colon and reduced inflammatory cell infiltration.
Decreased the levels of TNF-α, IL-1β, and IL-6 in colonic tissues and serum.
Restored gut microbial diversity, increased the abundances of Alistipes and Duncaniella, and suppressed the overgrowth of Akkermansia.
Promoted the production of short-chain fatty acids (acetic acid, propionic acid, and butyric acid) in the cecum.
Modulated host metabolic pathways, including purine metabolism, amino acid metabolism, and steroid hormone biosynthesis.
Chemical Information
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CAS No. 81840-57-5
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Appearance Solid
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Masse moléculaire 310.39
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Formule C20H22O3
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Color Off-white to light yellow
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SMILES
O=C(CCCCC1=CC=CC=C1)/C=C/C2=CC(OC)=C(C=C2)O
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Structure Classification
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Initial Source
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
-20°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvant et solubilité
In Vitro:
DMSO : 50 mg/mL (161.09 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1.25 mg/mL (4.03 mM); Clear solution
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1.25 mg/mL (4.03 mM); Clear solution
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
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 (protect from light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Pureté et documentation
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Fiche technique (286 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
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 (protect from light). 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 | 3.2218 mL | 16.1088 mL | 32.2175 mL | 80.5438 mL |
| 5 mM | 0.6444 mL | 3.2218 mL | 6.4435 mL | 16.1088 mL | |
| 10 mM | 0.3222 mL | 1.6109 mL | 3.2218 mL | 8.0544 mL | |
| 15 mM | 0.2148 mL | 1.0739 mL | 2.1478 mL | 5.3696 mL | |
| 20 mM | 0.1611 mL | 0.8054 mL | 1.6109 mL | 4.0272 mL | |
| 25 mM | 0.1289 mL | 0.6444 mL | 1.2887 mL | 3.2218 mL | |
| 30 mM | 0.1074 mL | 0.5370 mL | 1.0739 mL | 2.6848 mL | |
| 40 mM | 0.0805 mL | 0.4027 mL | 0.8054 mL | 2.0136 mL | |
| 50 mM | 0.0644 mL | 0.3222 mL | 0.6444 mL | 1.6109 mL | |
| 60 mM | 0.0537 mL | 0.2685 mL | 0.5370 mL | 1.3424 mL | |
| 80 mM | 0.0403 mL | 0.2014 mL | 0.4027 mL | 1.0068 mL | |
| 100 mM | 0.0322 mL | 0.1611 mL | 0.3222 mL | 0.8054 mL |
Yakuchinone B Related Classifications
HY-169813 Related Classifications
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