Anti-inflammatory agent 99
Based on 1 Customer Validation
Anti-inflammatory agent 99 is a chalcone derivative. Anti-inflammatory agent 99 inhibits LPS (HY-D1056)-induced NF-κB nuclear translocation and suppress the phosphorylation of JNK, ERK, and p38. Anti-inflammatory agent 99 inhibits the expression of cytoinflammatory factors such as TNF-α and IL-6 induced by LPS. Anti-inflammatory agent 99 can be used for the research of LPS-induced septic shock.
For research use only. We do not sell to patients.
- Purity : 98.65%
- CAS No.: 1345412-48-7
- Formula: C16H12F2O2
- Molecular Weight:274.26
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
JNK |
NF-κB |
p38 |
ERK |
IL-6 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| RAW264.7 | IC50 |
5.55 μM
Compound: 26
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Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced IL6 production incubated for 2 hrs prior to LPS-challenge measured after 22 hrs by ELISA
Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced IL6 production incubated for 2 hrs prior to LPS-challenge measured after 22 hrs by ELISA
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[PMID: 21988173] |
| RAW264.7 | IC50 |
8.42 μM
Compound: 26
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Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced TNFalpha production incubated for 2 hrs prior to LPS-challenge measured after 22 hrs by ELISA
Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced TNFalpha production incubated for 2 hrs prior to LPS-challenge measured after 22 hrs by ELISA
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[PMID: 21988173] |
In Vitro
Anti-inflammatory agent 99 (Compound 26) (2.5-10 μM; 24 h) dose-dependently inhibits LPS-induced TNF-α and IL-6 release in mouse RAW 264.7 macrophages, with IC50 values of 8.42 μM and 5.55 μM, respectively[1].
Anti-inflammatory agent 99 (10 μM; 8 h) inhibits LPS-induced TNF-α, IL-6, IL-1β, and IL-12 mRNA expression in mouse primary peritoneal macrophages, but does not significantly reduce COX-2 mRNA levels[1].
Anti-inflammatory agent 99 (2.5-20 μM; 2.5-3 h) inhibits LPS-induced NF-κB p65 nuclear translocation, and dose-dependently prevents LPS-induced IκB degradation in mouse primary peritoneal macrophages[1].
Anti-inflammatory agent 99 (2.5-20 μM; 2.5 h) dose-dependently inhibits LPS-induced JNK phosphorylation in mouse primary peritoneal macrophages[1].
Anti-inflammatory agent 99 (2.5-20 μM; 3 h) inhibits LPS-induced ERK and p38 phosphorylation, and dose-dependently blocks LPS-induced p38 and ERK activation in mouse primary peritoneal macrophages[1].
Anti-inflammatory agent 99 (10 μM; 5 h) inhibits high Glucose (HY-B0389)-induced TNF-α, IL-1β, IL-6, and IL-12 mRNA expression in mouse primary peritoneal macrophages[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:mouse RAW 264.7 macrophages
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Concentration:2.5 μM; 5.0 μM; 10 μM
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Incubation Time:24 h
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Result:Dose-dependently inhibited LPS-induced TNF-α and IL-6 release.
Exhibited an IC50 of 8.42 μM for TNF-α inhibition and an IC50 of 5.55 μM for IL-6 inhibition.
Significantly reduced TNF-α and IL-6 levels compared to the LPS-only group at 10 μM (p < 0.01).
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Cell Line:mouse primary peritoneal macrophages
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Concentration:10 μM
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Incubation Time:8 h
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Result:Inhibits LPS-induced TNF-α, IL-6, IL-1β, and IL-12 mRNA expression.
Did not significantly reduce COX-2 mRNA levels.
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Cell Line:mouse primary peritoneal macrophages
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Concentration:10 μM
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Incubation Time:2.5 h
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Result:Inhibited LPS-induced NF-κB p65 nuclear translocation.
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Cell Line:mouse primary peritoneal macrophages
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Concentration:2.5 μM; 5 μM; 10 μM; 20 μM
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Incubation Time:3 h
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Result:Dose-dependently inhibited LPS-induced IκB degradation, JNK phosphorylation and activation of p38 and ERK.
Inhibited LPS-induced ERK and p38 phosphorylation at 10 μM.
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Cell Line:mouse primary peritoneal macrophages
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Concentration:10 μM
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Incubation Time:5 h
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Result:Inhibited high Glucose-induced TNF-α, IL-1β, IL-6, and IL-12 mRNA expression.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 (B6) (male, 18−22 g, LPS-induced inflammatory shock model)[1]
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Dosage:15 mg/kg
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Administration:i.v.; single dose
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Result:Exhibited an 80% survival rate over the 7-day observation period.
Showed body weight decrease during the first 60 hours after LPS treatment that regained slowly afterward.
Chemical Information
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CAS No. 1345412-48-7
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Appearance Solid
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Molecular Weight 274.26
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Formula C16H12F2O2
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SMILES
O=C(C1=CC=C(C=C1)OC)/C=C/C2=C(C=CC=C2F)F
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (364.62 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.
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.
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 (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.
Purity & Documentation
References
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 | 3.6462 mL | 18.2309 mL | 36.4618 mL | 91.1544 mL |
| 5 mM | 0.7292 mL | 3.6462 mL | 7.2924 mL | 18.2309 mL | |
| 10 mM | 0.3646 mL | 1.8231 mL | 3.6462 mL | 9.1154 mL | |
| 15 mM | 0.2431 mL | 1.2154 mL | 2.4308 mL | 6.0770 mL | |
| 20 mM | 0.1823 mL | 0.9115 mL | 1.8231 mL | 4.5577 mL | |
| 25 mM | 0.1458 mL | 0.7292 mL | 1.4585 mL | 3.6462 mL | |
| 30 mM | 0.1215 mL | 0.6077 mL | 1.2154 mL | 3.0385 mL | |
| 40 mM | 0.0912 mL | 0.4558 mL | 0.9115 mL | 2.2789 mL | |
| 50 mM | 0.0729 mL | 0.3646 mL | 0.7292 mL | 1.8231 mL | |
| 60 mM | 0.0608 mL | 0.3038 mL | 0.6077 mL | 1.5192 mL | |
| 80 mM | 0.0456 mL | 0.2279 mL | 0.4558 mL | 1.1394 mL | |
| 100 mM | 0.0365 mL | 0.1823 mL | 0.3646 mL | 0.9115 mL |
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