PDE4B-IN-2
Based on 1 Customer Validation
PDE4B-IN-2 is an orally active and selective PDE4B inhibitor with an IC50 of 15 nM. PDE4B-IN-2 inhibits PDE4D (IC50=1.7 μM). PDE4B-IN-2 exhibits potent anti-inflammatory effects.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 99.59%
- CAS. Nr.: 915082-52-9
- Formel: C19H18ClN3O2S
- Molecular Weight:387.88
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Protokoll
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
PDE4B 15 nM (IC50) |
PDE4D 1.7 μM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| PBMC | IC50 |
0.5 M
Compound: 33
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Inhibition of LPS-induced TNFalpha production in mouse PBMCs
Inhibition of LPS-induced TNFalpha production in mouse PBMCs
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[PMID: 19447034] |
| Sf9 | IC50 |
32 nM
Compound: 16; CHEMBL1782306
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Inhibition of human N-terminal His6-tagged PDE4B1 catalytic domain (324 to 691 residues) expressed in baculovirus infected sf9 cells using cAMP as substrate preincubated for 15 mins followed by substrate addition measured for 10 mins in presence of NADH b
Inhibition of human N-terminal His6-tagged PDE4B1 catalytic domain (324 to 691 residues) expressed in baculovirus infected sf9 cells using cAMP as substrate preincubated for 15 mins followed by substrate addition measured for 10 mins in presence of NADH b
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[PMID: 26908025] |
In Vitro
PDE4B-IN-2 (compound 33) does not inhibit CYP1A2, CYP3A4, CYP2C9, and CYP2D (IC50>10 μM)[1].
PDE4B-IN-2 inhibits LPS-induced TNF-aproduction in vitro from mouseperipheral blood mononuclear cell (PBMC; IC50=0.5 M)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 915082-52-9
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Appearance Solid
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Molecular Weight 387.88
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Formel C19H18ClN3O2S
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Color White to off-white
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SMILES
O=C(O)CC1=CC=C(NC2=NC(C3=CC=C(Cl)S3)=NC(C)=C2CC)C=C1
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 25 mg/mL (64.45 mM; ultrasonic and warming and heat to 60°C; 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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Protokoll
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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
Reinheit & Dokumentation
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Data Sheet (270 KB)
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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)
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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. 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 | 2.5781 mL | 12.8906 mL | 25.7812 mL | 64.4529 mL |
| 5 mM | 0.5156 mL | 2.5781 mL | 5.1562 mL | 12.8906 mL | |
| 10 mM | 0.2578 mL | 1.2891 mL | 2.5781 mL | 6.4453 mL | |
| 15 mM | 0.1719 mL | 0.8594 mL | 1.7187 mL | 4.2969 mL | |
| 20 mM | 0.1289 mL | 0.6445 mL | 1.2891 mL | 3.2226 mL | |
| 25 mM | 0.1031 mL | 0.5156 mL | 1.0312 mL | 2.5781 mL | |
| 30 mM | 0.0859 mL | 0.4297 mL | 0.8594 mL | 2.1484 mL | |
| 40 mM | 0.0645 mL | 0.3223 mL | 0.6445 mL | 1.6113 mL | |
| 50 mM | 0.0516 mL | 0.2578 mL | 0.5156 mL | 1.2891 mL | |
| 60 mM | 0.0430 mL | 0.2148 mL | 0.4297 mL | 1.0742 mL |
PDE4B-IN-2 Related Classifications
HY-115687 Related Classifications
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