PDE4B-IN-3
Based on 1 Customer Validation
PDE4B-IN-3 is a potent PDE4B inhibitor with an IC50 of 0.94 μM. PDE4B-IN-3 has anti-inflammatory activities.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度 : 99.37%
- CAS 番号: 2819779-01-4
- 分子式: C30H35N3O4S2
- 分子量:565.75
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
生物活性
製品説明
IC50 & Target
[1]|
PDE4B .94 μM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| RAW264.7 | IC50 |
18.98 μM
Compound: f4
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Anti-inflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced IL-1beta production measured after 24 hrs by ELISA
Anti-inflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced IL-1beta production measured after 24 hrs by ELISA
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[PMID: 35660249] |
| RAW264.7 | IC50 |
20.4 μM
Compound: f4
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Inhibition of LPS induced NO production in mouse RAW264.7 cells preincubated for 1 hr followed by LPS addition and measured after 24 hrs by Griess reagent based assay
Inhibition of LPS induced NO production in mouse RAW264.7 cells preincubated for 1 hr followed by LPS addition and measured after 24 hrs by Griess reagent based assay
|
[PMID: 35660249] |
| RAW264.7 | IC50 |
23.48 μM
Compound: f4
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Anti-inflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced TNF-alpha production measured after 24 hrs by ELISA
Anti-inflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced TNF-alpha production measured after 24 hrs by ELISA
|
[PMID: 35660249] |
体外実験
PDE4B-IN-3 (compound f4) has good inhibitory activity on the production of NO, TNF-α and IL-1β with IC50 values of 20.40 μM, 23.48 μM, and 18.98 μM in RAW264.7 cells. PDE4B-IN-3 could also inhibit the expression of iNOS and COX-2 in RAW264.7 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 2819779-01-4
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性状 Solid
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分子量 565.75
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分子式 C30H35N3O4S2
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Color White to off-white
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SMILES
CC(C1=CC(C(C)C)=C(C(C(C)C)=C1)S(=O)(NC2=CC(NS(=O)(C3=CC=CC4=CC=CN=C43)=O)=CC=C2)=O)C
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
体外:
DMSO : 50 mg/mL (88.38 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. 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
体内:
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 (4.42 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.
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.
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.
プロトコル
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Research Protocol for Inflammation-related Diseases
The NLRP3 inflammasome is a cytosolic innate immune signaling platform that integrates priming signals and danger-signal activation to promote caspase-1 activation, maturation of IL-1β and IL-18, and gasdermin D-mediated pyroptotic cell death. The core experimental logic is to determine whether inflammatory disease phenotypes are driven by increased NLRP3 expression, ASC-containing inflammasome assembly, caspase-1 cleavage, GSDMD cleavage, and extracellular release of IL-1β/IL-18 rather than by nonspecific cell injury alone. The pathway is strongly linked to inflammation-related disease phenotypes because monosodium urate crystals activate NALP3/NLRP3 inflammasome signaling in gout-like crystal inflammation, cholesterol crystals activate NLRP3 inflammasomes in atherogenesis models, and DSS-induced intestinal inflammation has been reported to involve NLRP3 inflammasome activity. However, experimental colitis studies also show context-dependent protective effects of NLRP3 inflammasome co
純度とドキュメンテーション
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データシート (275 KB)
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SDS (251 KB)
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- Français - FR (251 KB)
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- Italian - IT (251 KB)
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- Portuguese - PT (251 KB)
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取扱説明書 (2659 KB)
参考文献
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. 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 | 1.7676 mL | 8.8378 mL | 17.6757 mL | 44.1891 mL |
| 5 mM | 0.3535 mL | 1.7676 mL | 3.5351 mL | 8.8378 mL | |
| 10 mM | 0.1768 mL | 0.8838 mL | 1.7676 mL | 4.4189 mL | |
| 15 mM | 0.1178 mL | 0.5892 mL | 1.1784 mL | 2.9459 mL | |
| 20 mM | 0.0884 mL | 0.4419 mL | 0.8838 mL | 2.2095 mL | |
| 25 mM | 0.0707 mL | 0.3535 mL | 0.7070 mL | 1.7676 mL | |
| 30 mM | 0.0589 mL | 0.2946 mL | 0.5892 mL | 1.4730 mL | |
| 40 mM | 0.0442 mL | 0.2209 mL | 0.4419 mL | 1.1047 mL | |
| 50 mM | 0.0354 mL | 0.1768 mL | 0.3535 mL | 0.8838 mL | |
| 60 mM | 0.0295 mL | 0.1473 mL | 0.2946 mL | 0.7365 mL | |
| 80 mM | 0.0221 mL | 0.1105 mL | 0.2209 mL | 0.5524 mL |