General description
A cell-permeable, brain permeant, quinoline-based compound that acts as a highly potent and selective inhibitor of phosphodiesterase 5 (PDEV; IC50 = 270 pM). Exhibits over 10,000 fold greater selectivity over various other phosphodiestrases and trivial activity against PDE VI (IC50 = 339 nM). Shown to increase cGMP levels in mouse hippocampus and attenuates long term potentiation and memory defects in mice with elevated levels of oligomeric Aβ42. It is rapidly absorbed with peak plasma concentration observed at 30 min. Displays desirable pharmacokinetic properties with plasma t1/2 = 1.33 h and brain t1/2 = 1.04 h.
A cell-permeable, brain permeant, quinoline-based compound that acts as a highly potent and selective inhibitor of phosphodiesterase 5 (PDEV; IC50 = 270 pM). Exhibits over 10,000 fold greater selectivity over various other phosphodiestrases and trivial activity against PDE VI (IC50 = 339 nM). Shown to increase cGMP levels in mouse hippocampus and attenuates long term potentiation and memory defects in mice with elevated levels of oligomeric Aβ42. It is rapidly absorbed with peak plasma concentration observed at 30 min. Displays desirable pharmacokinetic properties with plasma t1/2 = 1.33 h and brain t1/2 = 1.04 h.
Please note that the molecular weight for this compound is batch-specific due to variable water content.
Biochem/physiol Actions
Primary Target
PDE5
Reversible: yes
Packaging
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Fiorito, J., et al. 2013. Eur. J. Med. Chem.60, 285.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Molecular Weight: 393.87. Empirical Formula: C22H20ClN3O2. Assay: ≥. 98% (HPLC). Quality Level: 100. form: solid. potency: 270 . pM IC50. manufacturer/tradename: Calbiochem®. . storage condition: OK to freeze, protect from light. color: cream. solubility: DMSO: 100 . mg/mL. storage temp.: 2-8°C. Storage Class Code: 11 - Combustible Solids. WGK: WGK 3. Flash Point(F): Not applicable. Flash Point(C): Not applicable.- UPC:
- 51142550
- Condition:
- New
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- 5089570001