PDE4B/7A-IN-1
Based on 1 Customer Validation
PDE4B/7A-IN-1 is a dual PDE4B/PDE7A inhibitor. PDE4B/7A-IN-1 shows IC50 values of 69.0 μM for PDE4B and 57.0 μM for PDE7A, as well as Ki values of 539 nM for 5-HT1A and 328 nM for 5-HT7. PDE4B/7A-IN-1 shows favorable membrane permeability. PDE4B/7A-IN-1 can be used for the study of cognitive impairment and depression.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 99.63%
- CAS. Nr.: 2511632-25-8
- Formel: C25H35N3O3
- Molecular Weight:425.56
-
Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Alle 5-HT Receptor Isoform-spezifische Produkte anzeigen
More
Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
PDE4B 69 μM (IC50) |
PDE7A 57 μM (IC50) |
5-HT7 Receptor 328 nM (Ki) |
5-HT1A Receptor 539 nM (Ki) |
5-HT1A Receptor 3.4 nM (Kb) |
5-HT7 Receptor 2300 nM (Kb) |
In Vitro
PDE4B/7A-IN-1 (compound 7) shows low affinity for human 5-HT1A receptors stably expressed in HEK293 cells, with a Ki of 539 nM[1].
PDE4B/7A-IN-1 shows moderate affinity for human 5-HT7 receptors stably expressed in HEK293 cells, with a Ki of 328 nM[1].
PDE4B/7A-IN-1 weakly inhibits PDE4B enzyme activity, with an IC50 of 69.0 μM[1].
PDE4B/7A-IN-1 weakly inhibits PDE7A enzyme activity, with an IC50 of 57.0 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Chemical Information
-
CAS. Nr. 2511632-25-8
-
Appearance Solid
-
Molecular Weight 425.56
-
Formel C25H35N3O3
-
Color White to off-white
-
SMILES
COC1=C(C=CC=C1)N2CCN(CC2)CCCC(NC3=CC(C(C)(C)C)=CC=C3O)=O
-
Versand
Room temperature in continental US; may vary elsewhere.
-
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 : 50 mg/mL (117.49 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
-
Transepithelial/transendothelial electrical resistance assay
TEER measures electrical resistance across epithelial or endothelial monolayers cultured on permeable supports, and the readout reflects ionic conductance through the cell barrier, especially the paracellular pathway regulated by junctional integrity. TEER can be measured without destroying the monolayer and is commonly used before or during transport, permeability, barrier-disruption, and barrier-maturation experiments. TEER values are influenced by biological maturation and technical conditions; reported factors include temperature, medium formulation, passage number, electrode geometry, membrane properties, and junctional length during early monolayer maturation. Therefore, TEER should be interpreted with blank-insert subtraction, area normalization, repeated readings, and, when possible, orthogonal barrier readouts such as FITC-dextran flux or tight-junction staining.
-
Alzheimer’s Disease Modeling
Alzheimer’s Disease (AD) is a neurodegenerative disorder characterized by a progressive decline in cognitive functions and loss of specific types of neurons and synapses. Alzheimer's symptoms can be simulated in mice by injecting drugs (such as Aβ) or genetically modified.
Reinheit & Dokumentation
-
Data Sheet (270 KB)
-
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)
-
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 | 2.3498 mL | 11.7492 mL | 23.4984 mL | 58.7461 mL |
| 5 mM | 0.4700 mL | 2.3498 mL | 4.6997 mL | 11.7492 mL | |
| 10 mM | 0.2350 mL | 1.1749 mL | 2.3498 mL | 5.8746 mL | |
| 15 mM | 0.1567 mL | 0.7833 mL | 1.5666 mL | 3.9164 mL | |
| 20 mM | 0.1175 mL | 0.5875 mL | 1.1749 mL | 2.9373 mL | |
| 25 mM | 0.0940 mL | 0.4700 mL | 0.9399 mL | 2.3498 mL | |
| 30 mM | 0.0783 mL | 0.3916 mL | 0.7833 mL | 1.9582 mL | |
| 40 mM | 0.0587 mL | 0.2937 mL | 0.5875 mL | 1.4687 mL | |
| 50 mM | 0.0470 mL | 0.2350 mL | 0.4700 mL | 1.1749 mL | |
| 60 mM | 0.0392 mL | 0.1958 mL | 0.3916 mL | 0.9791 mL | |
| 80 mM | 0.0294 mL | 0.1469 mL | 0.2937 mL | 0.7343 mL | |
| 100 mM | 0.0235 mL | 0.1175 mL | 0.2350 mL | 0.5875 mL |