ASB14780
Based on 1 publication(s) in Google Scholar
ASB14780 is a 4-phenoxy derivative, the cytosolic Phospholipase A2α (cPLA2α) inhibitor, with an IC50 value of 20 nM.
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- Reinheit: 99.58%
- CAS. Nr.: 1069046-00-9
- Formel: C35H38N2O6
- Molecular Weight:582.69
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Speicherung:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) ASB14780
More
Biologische Aktivität
IC50: 20 nM (cPLA2α); 0.54 μM (guinea pig cPLA2α); 0.64 μM (human cPLA2α)[1]
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Cell Line
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Type | Value | Description | References |
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| U-937 | IC50 |
0.02 μM
Compound: 56n
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Inhibition of cPLA2alpha isolated from human U937 cell cytoplasm assessed as suppression of [14C]arachidonic acid release from L-alpha-1-palmitoyl-2-[14C]arachidonyl-phosphatidylcholine liposomes substrate by scintillation counting
Inhibition of cPLA2alpha isolated from human U937 cell cytoplasm assessed as suppression of [14C]arachidonic acid release from L-alpha-1-palmitoyl-2-[14C]arachidonyl-phosphatidylcholine liposomes substrate by scintillation counting
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[PMID: 25102418] |
ASB14780 shows selectivity to cPLA2α (IC50 =20 nM) over type II sPLA2 (IC50 >10 μM)[1].
ASB14780 (30 min pre-incucation) inhibits cPLA2α in guinea pig whole blood (GWB) and human whole blood (HWB) in a species-derived differences, with IC50s of 0.54 μM and 0.64 μM, respectively, 15 min after being stimulated by 5 μM calcium ionophore A23187[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
ASB14780 (50 mg/kg; p.o.; once) suppresses the increase in the ear thickness elicited by the application of TPA (tetradecanoyl phorbol acetate) in mouse[1].
ASB14780 (5 mg/kg; 20 mg/kg; p.o.; once daily) attenuates AHR (airway hyperreactivity), and inhibits IAR (immediate asthmatic response) and LAR (late asthmatic response) in a dose-dependent manner[1].
ASB14780 shows well oral activity of 89.6% in mouse calculated from the ratio of oral administration’s AUC (10 mg/kg; p.o.) and intravenonous administration’s AUC (1 mg/kg; i.v.)[1].
Oral Bioavailabilities and Pharmacokinetic Parameters of ASB14780[1]
| Model | F (%) | AUC (h μg/mL) | Cmax (μg/mL) |
| mouse | 89.6 | 7.12 | 5.12 |
| dog | 34.3 | 17.1 | 4.96 |
| monkey | 30.9 | 4.96 | 2.29 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:TPA (Tetradecanoyl Phorbol Acetate)-induced Ear Edema Model in mouse (female C57BL/6 mice)[1]
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Dosage:50 mg/kg
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Administration:Oral gavage; 30 min before TPA stimulation
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Result:Showed high potency and inhibited ear swelling by 30% and indicated the in vivo anti-inflammatory activity.
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Animal Model:Guinea Pig Ovalbumin (OVA)-induced Asthma Model[1]
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Dosage:5 mg/kg, 20 mg/kg
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Administration:Oral gavage; two single doses; 1 h before and 8 h after passively sensitized administration
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Result:Exhibits suppression on IAR (immediate asthmatic response) and LAR (late asthmatic response) in a dose-dependent manner.
Chemical Information
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CAS. Nr. 1069046-00-9
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Appearance Solid
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Molecular Weight 582.69
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Formel C35H38N2O6
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Color White to off-white
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SMILES
O=C(CCC1=CC(C(CCC2=CC=CC=C2)=CN3C4=CC=C(C=C4)OC5=CC=CC=C5)=C3C=C1)O.OCC(CO)(CO)N
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (1)
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Journal Impact Factor
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Most Recent
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FASEB J
Mechano-induced arachidonic acid metabolism promotes keratinocyte proliferation through cPLA2 activity regulation. [Abstract]2024 Dec 15;38(23):e70226. PMID: 39636236
Lösungsmittel & Löslichkeit
DMSO : 100 mg/mL (171.62 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 (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.
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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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: ≥ 2.5 mg/mL (4.29 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 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.
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 (sealed storage, away from moisture)
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.
Reinheit & Dokumentation
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Data Sheet (291 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)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
Verweise
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 | 1.7162 mL | 8.5809 mL | 17.1618 mL | 42.9045 mL |
| 5 mM | 0.3432 mL | 1.7162 mL | 3.4324 mL | 8.5809 mL | |
| 10 mM | 0.1716 mL | 0.8581 mL | 1.7162 mL | 4.2904 mL | |
| 15 mM | 0.1144 mL | 0.5721 mL | 1.1441 mL | 2.8603 mL | |
| 20 mM | 0.0858 mL | 0.4290 mL | 0.8581 mL | 2.1452 mL | |
| 25 mM | 0.0686 mL | 0.3432 mL | 0.6865 mL | 1.7162 mL | |
| 30 mM | 0.0572 mL | 0.2860 mL | 0.5721 mL | 1.4301 mL | |
| 40 mM | 0.0429 mL | 0.2145 mL | 0.4290 mL | 1.0726 mL | |
| 50 mM | 0.0343 mL | 0.1716 mL | 0.3432 mL | 0.8581 mL | |
| 60 mM | 0.0286 mL | 0.1430 mL | 0.2860 mL | 0.7151 mL | |
| 80 mM | 0.0215 mL | 0.1073 mL | 0.2145 mL | 0.5363 mL | |
| 100 mM | 0.0172 mL | 0.0858 mL | 0.1716 mL | 0.4290 mL |
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